СПОСОБ И УСТРОЙСТВО ДЛЯ ПОЛУЧЕНИЯ МОЧЕВИНОВОЙ КОНСИСТЕНТНОЙ СМАЗКИ

Изобретение относится к способу получения мочевиновой консистентной смазки, который осуществляют в устройстве, использующем экструдер и содержащем несколько реакционных зон, смонтированных в ряд и связанных по текучей среде. При этом устройство включает в себя: (а) первую зону подачи; (b) вторую зону подачи; (с) первую зону реакции-смешивания и (d) зону охлаждения-смешивания, причем указанные зоны расположены в устройстве в порядке (а), (b), (с), (d), и способ включает введение первого исходного компонента в первую зону подачи (а); введение второго исходного компонента во вторую зону подачи (b); реакцию первого и второго компонентов в первой зоне реакции-смешивания (с) и охлаждение и смешивание продукта первой зоны реакции-смешивания в зоне охлаждения-смешивания (d) с получением мочевиновой консистентной смазки. Также изобретение относится к устройству для осуществления данного способа. Настоящее изобретение обладает такими преимуществами, как технологическая стабильность, обладает трансформируемостью ...

СПОСОБ ПОЛУЧЕНИЯ N-НИТРОЗО-N-[(2-ХЛОРЭТИЛ)КАРБАМОИЛ]-L-ОРНИТИНА

Изобретение относится к способу получения N-нитрозо-N-[(2-хлорэтил)карбамоил]-L-орнитина формулы, обладающего противоопухолевым действием. Согласно предлагаемому способу N-нитрозо-N-[(2-хлорэтил)карбамоил]-L-орнитин получают из смеси изомеров N-нитрозо-N-[(2-хлорэтил)карбамоил]-L-орнитина и N-[(2-хлорэтил)-N-нитрозокарбамоил]-L-орнитина, при этом раствор смеси изомеров в воде выдерживают в течение 50 ч при +37°С, концентрируют реакционную массу и выдерживают 8 ч при +8°С. Предлагаемый способ не требует сложного аппаратурного оформления и позволяет за один цикл получать значительные количества целевого продукта. 1 ил., 1 табл., 1 пр.

СПОСОБ СИНТЕЗА (Z)-3-[2-БУТОКСИ-3'-(3-ГЕПТИЛ-1-МЕТИЛУРЕИДО)БИФЕНИЛ-4-ИЛ]-2-МЕТОКСИАКРИЛОВОЙ КИСЛОТЫ

... 1. Способ синтеза (Z)-3-[2-бутокси-3'-(3-гептил-1-метилуреидо)бифенил-4-ил]-2-метоксиакриловой кислоты формулы (I) ! ! отличающийся тем, что сульфонат общей формулы (XII) ! , ! где R2 означает метил, трифторметил, фенил или толил, подвергают взаимодействию с 3-гептил-1-метил-1-[3-(4,4,5,5-тетраметил[1,3,2]диоксаборолан-2-ил)фенил]мочевиной формулы (IIIb) ! ! или с соответствующей бороновой кислотой формулы (IIIa) ! ! 2. Способ по п.1, отличающийся тем, что реакцию проводят в присутствии палладиевого или никелевого катализатора. ! 3. Способ по п.1 или 2, отличающийся тем, что сульфонат общей формулы (XII) ! ! получают омылением сложного эфира общей формулы (XIII) ! ! где R1 означает алкил. ! 4. Способ по п.3, отличающийся тем, что сложный эфир общей формулы (XIII) ! ! получают взаимодействием алкил (Z)-3-(3-бутокси-4-гидроксифенил)-2-метоксиакрилата общей формулы (XIV) ! ! с соединением, выбранным из трифлик ангидрида, мезилхлорида, бензолсульфонилхлорида и тозилхлорида. ! 5. Способ по п ...

Epoxidation of glycerol and derivatives therefrom

EPOXIDATION OF GLYCEROL AND DERIVATIVES THEREFROM

Epoxidation of glycerol and derivatives therefrom

Epoxidation of glycerol and derivatives therefrom

Cyclic peptidomimetic compounds as immunomodulators

The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also 5 encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-Li, or PD-L2 and therapies using them.

Process for producing guanidine derivatives, intermediates therefor and their production

Verfahren zur Herstellung von polyhalogensubstituierten Monooxydiphenylharnstoff- und -thioharnstoffverbindungen

ЗАМЕЩЕННЫЕ ПИРАЗОЛЫ, КОМПОЗИЦИИ, ИХ СОДЕРЖАЩИЕ, СПОСОБ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ

Настоящее изобретение относится к новым химическим соединениям, в особенности к замещенным пиразолам, композициям их содержащим и их применению в качестве лекарственных средств.

ЗАМЕЩЕННЫЕ ПИРАЗОЛЫ, СОДЕРЖАЩАЯ ИХ КОМПОЗИЦИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

Данное изобретение касается химических соединений, особенно замещенных пиразолов, содержащих их композиций, и их применения в качестве лекарственных средств.

METHOD OF PREPARING COMPOUNDS, USED IN CYCLIC PEPTIDOMIMETIChESKIKh COMPOUNDS

METHOD OF PREPARING COMPOUNDS, USED IN CYCLIC PEPTIDOMIMETIChESKIKh COMPOUNDS

ЗАМЕЩЕННЫЕ ПИРАЗОЛЫ, КОМПОЗИЦИИ ИХ СОДЕРЖАЩИЕ, СПОСОБ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ

Изобретение относится к замещенным пиразолам общей формулы (I), композициям, их содержащим, и их применению в качестве лекарственных средств для лечения рака.

PYRAZOLES SUBSTITUEES, COMPOSITIONS THE CONTAINER, MANUFACTORING PROCESS AND USE

Process for the production of derived from urea

Processo para produzir compostos ou um seu sal e composto

ЭТИЛОВЫЙ ЭФИР 2-{ 4-[3-(4-ХЛОРФЕНИЛ)-1-МЕТИЛУРЕИДО]ФЕНИЛ} -2-ГИДРОКСИ-3,3,3-ТРИФТОРПРОПИОНОВОЙ КИСЛОТЫ: ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИДОТА ГЕРБИЦИДОВ И СПОСОБ ПОЛУЧЕНИЯ

FIELD: chemistry.SUBSTANCE: invention relates to the use of ethyl ester 2-{4-[3-(4-chlorophenyl)-1-methylureido]phenyl}-2-hydroxy-3,3,3-trifluoropropionic acid of the formula I in agriculture as an antidote of methylsulfuron methyl on rapeseed for presowing seed treatment. Compound of formula I is used at a dosage of 1 g/ton of seeds..EFFECT: processing of rapeseed seeds with said antidote effectively attenuates the toxic effect of the herbicide and leads to an increase in the overground weight of the plants.1 cl, 1 tbl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 666 732 C1 (51) МПК C07C 273/18 (2006.01) C07C 275/42 (2006.01) A01N 25/32 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 273/18 (2006.01); C07C 275/42 (2006.01); A01N 25/32 (2006.01) (21)(22) Заявка: 2017125487, 17.07.2017 (24) Дата начала отсчета срока действия патента: Дата регистрации: 12.09.2018 (45) Опубликовано: 12.09.2018 Бюл. № 26 Адрес для переписки: 119991, Москва, В-334, ГСП-1, ул. Вавилова, 28, ИНЭОС РАН, отдел интеллектуальной собственности 27.03.2017). База данных PubChem [онлайн] NCBI; номер CID 2817877 (дата создания 19.07.2005). SU 1804056 A1, 20.11.1996. EP 0435840 A2, 03.07.1991. C 1 2 6 6 6 7 3 2 (56) Список документов, цитированных в отчете о поиске: CAS RN 292854-58-1 (опубл. (54) ЭТИЛОВЫЙ ЭФИР 2-{ 4-[3-(4-ХЛОРФЕНИЛ)-1-МЕТИЛУРЕИДО]ФЕНИЛ} -2-ГИДРОКСИ-3,3,3ТРИФТОРПРОПИОНОВОЙ КИСЛОТЫ: ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИДОТА ГЕРБИЦИДОВ И СПОСОБ ПОЛУЧЕНИЯ (57) Реферат: Изобретение относится к применению ослабляет токсическое действие гербицида и этилового эфира 2-{4-[3-(4-хлорфенил)-1приводит к увеличению надземной массы метилуреидо]фенил}-2-гидрокси-3,3,3растений. 1 з.п. ф-лы, 1 табл., 2 пр. трифторпропионовой кислоты формулы I в сельском хозяйстве в качестве антидота метсульфуронметила на рапсе для предпосевной обработки семян. Соединение формулы I применяют в дозе 1 г/т семян. Обработка семян рапса указанным антидотом ...

СТАБИЛЬНЫЕ ЖИДКИЕ МОДИФИЦИРОВАННЫЕ БИУРЕТНЫМИ И МОДИФИЦИРОВАННЫЕ БИУРЕТНЫМИ И АЛЛОФАНАТНЫМИ ГРУППАМИ ТОЛУОЛДИИЗОЦИАНАТЫ, ИХ ПРЕПОЛИМЕРЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ

... 1. Стабильный жидкий модифицированный биуретными группами толуолдиизоцианат, включающий основанный на вторичном амине модифицированный биуретными группами толуолдиизоцианат, обладающий содержанием групп NCO, равным от 16 до 46 мас.%, включающий (a) содержащее вторичную моноаминную группу соединение, которое может быть алифатическим, ароматическим или арилалифатическим; и (b) толуолдиизоцианат, обладающий содержанием групп NCO, равным примерно 48,3%, и включающий (i) от 0 до 40 мас.% 2,6-толуолдиизоцианата и (ii) от 60 до 100 мас.% 2,4-толуолдиизоцианата, где выраженные в мас.% содержания компонентов (b) (i) и (b) (ii) в сумме составляют 100 мас.% (b). 2. Стабильный жидкий модифицированный толуолдиизоцианат по п.1, в котором содержание групп NCO составляет от 20 до 40 мас.%. 3. Стабильный жидкий модифицированный биуретными группами толуолдиизоцианат по п.1, в котором (а) указанное содержащее вторичную моноаминную группу соединение обладает молекулярной массой, равной от примерно 45 до примерно ...

Verfahren zur Herstellung von Urethanen

Die Erfindung betrifft ein Verfahren zur Herstellung von Urethanen durch oxidative Carbonylierung von Aminoverbindungen in Gegenwart von Kohlenmonoxid, Sauerstoff und organischen, Hydroxylgruppen tragenden Verbindungen, dadurch gekennzeichnet, dass die Carbonylierung in Abwesenheit von halogenhaltigen Promotoren und in Anwesenheit von Metallkomplexkatalysatoren durchgeführt wird, die neutrale zweizähnige N-Chelatliganden des Typs (N ~ N), zwei mono-anionische N,O-Chelatliganen des allgemeinen Typs (N ~ O)- oder vierzähnige dianionische Chelatliganden (O ~ N ~ N ~ O)2- enthalten.

ARYLOXYCYCLOALKENYL- UND ARYLOXYIMINOCYCLOALKENYL-HYDROXYHARNSTOFFE MIT 5-LIPOXYGENASE INHIBIERENDER WIRKUNG

ISO THIOUREAS.

PROCEDURE FOR THE N-ALKYLATION OF UREA.

SUBSTITUTED 1,3-DIAMINOPROPANES

SUBSTITUTED 1,3-DIAMINOPROPANES N'-Acyl-N-alkyl-1,3-diaminopropanes of formula R1CONH(CH2)3NHR2 where R1 is R- or RNH where R is a substituted or unsubstituted hydrocarbon group and R2 is alkyl) are prepared by selectively acylating N-alkyl-1,3-diaminopropanes. In the process a N-alkyl 1,3-aminopropane is reacted with an aldebyde to form a hexahydropyrimidine, the hexahydropyrimidine is acylated and the acylated hexahydropyrimidine is then hydrolysed to give the product.

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

Substituted pyrazoles, compositions containing these, method of production and use

The present invention relates to new chemical compounds, particularly to substituted pyrazoles, compositions containing these, and their use as drugs.

Method of making metal substituted urea

Composition, manufacturing method of the same, and manufacturing method of unsaturated compound

Provided is a compound: including a compound A represented by the general formula (1) and a compound B represented by the general formula (2), wherein the compound B is included in an amount of 0.00002 to 0.2 part by mass with respect to 100 part by mass of the compound A; (R1-COO)n-R2-(NCO)m(1) (R1-COO)n-R2-NHC(=o)NH-R2-(OCO-R1)m...(2) (in the general formula (1) and (2), R1 represents an ethylenically unsaturated group having 2 to 7 carbons, R2 represents a m+n valent hydrocarbon group having 1 to 7 carbons, wherein n and m are integers of 1 or 2, which may include an ether group.) (in the general formula (1) and (2), R1 and R2 are the same in each formula.).

METHOD FOR PRODUCING URETHANES

The invention relates to a method for producing urethanes by the oxidative carbonylation of amino compounds in the presence of carbon monoxide, oxygen and organic compounds carrying hydroxyl groups, characterized in that the carbonylation is carried out in the absence of promoters containing halogen and in the presence of metal complex catalysts containing neutral bidentate N-chelate ligands of the type (N~N), two monoanionic N,O- chelate ligands of the common type (N~O)-or tetradentate dianionic chelate ligands (O~N~N~O)2-.

Cyclic Peptidomimetic Compounds as Immunomodulators

The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 1140-. (canceled)141. A compound chosen from N-(4′-((trans)-2-((4-aminocyclohexyl)amino) cyclopropyl)-[1 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide , an optically active stereoisomer thereof , and a salt or solvate thereof.142. The compound of claim 141 , wherein the compound is an optically active stereoisomer.143. The compound of claim 141 , wherein the compound is N-(4′-((trans)-2-((4-aminocyclohexyl)amino) cyclopropyl)-[1 claim 141 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide or a pharmaceutically acceptable salt or solvate thereof.144. The compound of claim 141 , wherein the compound is a hydrochloride salt of N-(4′-((trans)-2-((4-aminocyclohexyl)amino) cyclopropyl)-[1 claim 141 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide.145. A pharmaceutical composition comprising a compound chosen from N-(4′-((trans)-2-((4-aminocyclohexyl)amino)cyclopropyl)-[1 claim 141 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide claim 141 , an optically active stereoisomer thereof claim 141 , and a pharmaceutically acceptable salt or solvate thereof claim 141 , and a pharmaceutically acceptable carrier.146. The pharmaceutical composition of claim 145 , wherein the compound is an optically active stereoisomer.147. The pharmaceutical composition of claim 145 , wherein the compound is N-(4′-((trans)-2-((4-aminocyclohexyl)amino)cyclopropyl)-[1 claim 145 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide or a pharmaceutically acceptable salt or solvate thereof.148. The pharmaceutical composition of claim 145 , wherein the compound is a hydrochloride salt of N-(4′-((trans)-2-((4-aminocyclohexyl)amino)cyclopropyl)-[1 claim 145 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide.149. A method of treating cancer ...

Cyclic peptidomimetic compounds as immunomodulators

Methods of making a compound according to the following scheme: wherein: R1is a side chain of an amino acid residue selected from Ala, Ser, Thr and Leu; R2is a side chain of an amino acid residue selected from Asp, Glu, Gln and Asn; [Aaa] is an amino acid residue selected from Ser, Asp, Ala, Ile, Phe, Trp, Lys, Glu and Thr; R3is hydrogen or alkyl; Each of R4and R4′ independently is hydrogen or alkyl; Both Raand Ra′ are hydrogen; or together are an oxo(═O) group; Both Rband Rb′ are hydrogen; or together are an oxo (═O) group; L is X is CH2, O or S; R5is hydrogen or alkyl; m is an integer from 1 to 3; and n is an integer from 2 to 20.

COMPOSITION, PRODUCTION METHOD FOR COMPOSITION, AND PRODUCTION METHOD FOR UNSATURATED COMPOUND

(ГЕТЕРО)АРИЛЦИКЛОПРОПИЛАМИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LSD1

Изобретение относится к новому (гетеро)арилциклопропиламину формулы I или его фармацевтически приемлемой соли, где заместители -А-В и -NH-D циклопропильного фрагмента могут находиться в транс-конфигурации или соединение может быть оптически активным стереоизомером. Соединения обладают свойствами ингибитора лизинспецифической деметилазы-1 (LSD1) и могут найти применение для лечения рака, выбранного из группы, включающей рак молочной железы, рак легких, рак предстательной железы, колоректальный рак, рак головного мозга, рак кожи, рак крови, лейкоз, лимфому и миелому. При этом лейкоз может представлять собой острый миелолейкоз (ОМЛ), хронический миелолейкоз (ХМЛ), хронический нейтрофильный лейкоз, хронический эозинофильный лейкоз, хронический лимфолейкоз (ХЛЛ), острый лимфобластный лейкоз (ОЛЛ) и волосатоклеточный лейкоз. Соединения также могут найти применение для лечения или предупреждения вирусной инфекции, в том числе для лечения или предупреждения реактивации вируса после латентного периода, который связан с LSD1. В соединении формулы IА обозначает фенил, нафтил, пиридил, тиофенил, пирролил, фуранил или тиазолил, где указанный фенил, указанный нафтил, указанный пиридил, указанный тиофенил, указанный пирролил, указанный фуранил или указанный тиазолил необязательно замещен одним или большим количеством R; В обозначает водород, Rили -L-E; Е обозначает фенил, пиридинил, пиразолил или индазолил, где указанный фенил, указанный пиридинил, указанный пиразолил или указанный индазолил необязательно замещен одним или большим количеством R; L обозначает связь, -О-, -NH-, -CH-NH- или -СН-О-, где указанные группы -CH-NH- и -СН-О- связаны с кольцом А через атом N или О соответственно и связаны с кольцом Е через группу -СН-, содержащуюся в указанных группах -CH-NH- и -СН-О-; D выбран из D1, D2, D3 и D4:где циклобутильное кольцо, содержащееся в D1, циклопентильное кольцо, содержащееся в D2, циклогексильное кольцо, содержащееся в D3, и циклогептильное кольцо, содержащееся в D4, ...

УЛУЧШЕННЫЙ СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ НИТРОИЗОМОЧЕВИНЫ

Изобретение относится к способу получения производных нитроизомочевины, представленных следующей общей формулой (3), в котором представленные следующей общей формулой (1) производные нитроизомочевины и представленные следующей общей формулой (2) амины или их соли взаимодействуют в присутствии каталитического количества гидрокарбоната ! ! При этом в формуле (1) R1 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода; ! ! в формуле (2) R2 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода, и R3 представляет собой атом водорода; ! ! в формуле (3) R1 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода; R2 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода; и R3 представляет собой атом водорода. Изобретение позволяет получить производные нитроизомочевины дешевым и легким способом. 7 з.п. ф-лы.

Verfahren zur Darstellung von Ureiden

VERFAHREN ZUR N-ALKYLIERUNG VON HARNSTOFFEN

Process for the N-alkylation of ureas by reacting a urea with an alkylating agent in the presence of a solid base and a phase transfer catalyst in a diluent.

PROCEDURE FOR THE PRODUCTION OF CARBAMOYLMETHYLHARNSTOFF DERIVATIVES

ARYLOXYCYCLOALKENYL AND ARYLOXYIMINOCYCLOALKENYL HYDROXYHARNSTOFFE ONES WITH 5-LIPOXYGENASE of INHIBIERENDER EFFECT

VERFAHREN ZUR N-ALKYLIERUNG VON HARNSTOFFEN

ALDIMIN HALTIGE CONNECTIONS

Use of monochlorourea to treat industrial waters

The present invention comprises a method for controlling (e.g. inhibiting) or killing microorganisms in an aqueous environment. The method includes the addition of an effective amount of monochlorourea or modified monochlorourea to an aqueous solution. This aqueous solution may be a cooling water system, a recreational water system, a water treatment facility, or any circulating water system (i.e. a papermaking facility). A method of producing monochlorourea or modified monochlorourea is also disclosed.

Aryloxycycloalkenyl and aryloxyiminocycloalkenylhydroxyureas

A NOVEL KCNQ POTASSIUM CHANNEL AGONIST, THE PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. (see above formula) ...

COMPOUNDS CONTAINING ALDIMINE

The invention relates to compounds of formula (I) which contain aldimine, and to the use thereof. Said compounds which contain aldimines are characterised in that they are odour-less and during hydrolysis the odour-free aldehydes are separated. They are used, therefor, as sources for aldehydes. They can also be used in cross-linking reactions.

ARYLOXYCYCLOALKENYL AND ARYLOXYIMINOCYCLOALKENYLHYDROXYUREAS AS 5-LIPOXYGENASE INHIBITORS

The present invention provides a compound of formula (I), wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C2-4 alkoxyalkoxy, C1-4 alkylthio, hydroxy, halo, cyano, amino, C1-4 alkylamino, di (C2-8) alkylamino, C2-6 alkanoylamino, carboxy, C 2- 6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo[b]furyl, thienyl, benzo[b]thienyl, pyridyl or quinolyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, halo, C1-4 alkoxy, optionally-substituted phenyl, phenoxy or phenylthio, X is C1-C4 alkylene, C2-C4 alkenylene, -(CHR1)m-Q1-(CHR2)n-, -O-(CHR1)j Q2- and -(CHR1)-O-N = in which the N = moie ty is attached to the cycloakene ring; and in which Q1 is O, S, SO, SO2, NR3, CH = N-O or CO, Q2 is O, S, SO, SO2 or NR3, and R1 , R2 and R3 are each hydrogen or C1-C4 alkyl, m and n are each an integer from 0 to 4 and j is an integer ...

Multifunctional polyurethane derivative containing triarylamine structure and tetrastyrene group as well as preparation method and application thereof.

Substituted pyrazoles, compositions containing these, method of production and use

The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.

СПОСОБ ПОЛУЧЕНИЯ N-АЛКИЛИРОВАННЫХ МОЧЕВИН

Использование: в сельском хозяйстве. Сущность изобретения: способ получения N-алкилированных мочевин ф-лы I: N(R1R2)-C(O)-NH(R3) , где R1 , R2 - независимо друг от друга - H или прямая или разветвленная алкильная группа; R1 и R2 вместе с атомом азота образуют неароматическое 5-6-членное кольцо; R - алкильная группа кроме трет-бутильной группы. Реагент 1: соединение формулы II: (R1R2)N-C(O)NH , где R1 и R2 имеют указанные значения. Реагент 2: (R3)nX , 0=1,2; X -галоид, сульфонокислотная или гидросульфатная группа при n = 1 или при n = 2 X -сульфатная группа. Условие реакции: процесс ведут в присутствии твердого основания и катализатора, способного к переносу фаз, такого как четвертичная аммонийная соль, в присутствии неполярного разбавителя или присутствии твердого основания и диметилсульфоксида. 5 з.п. ф-лы.

ПОЛИАМИДОМОЧЕВИННЫЕ ПРОИЗВОДНЫЕ ДИМЕРИЗОВАННОЙ ЖИРНОЙ КИСЛОТЫ

FIELD: chemistry. SUBSTANCE: invention relates to preparation of new derivatives of dimerized fatty acid, namely its polyamide ureal derivatives which can be used as heat-resistant hot melt adhesives. Polyamide ureal derivatives of dimerized fatty acid have a general structural formula where or HN(CH 2 ) 6 NH; where n=1. EFFECT: invention allows to obtain hot melt adhesives with high adhesive strength at high operating temperatures of glued products, and chemical resistance of adhesive joints. 2 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 616 298 C1 (51) МПК C07D 295/00 (2006.01) C07C 273/18 (2006.01) C07C 275/18 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2016109533, 16.03.2016 (24) Дата начала отсчета срока действия патента: 16.03.2016 Дата регистрации: (45) Опубликовано: 14.04.2017 Бюл. № 11 Адрес для переписки: 606000, Нижегородская обл., г. Дзержинск, ФГУП "НИИ полимеров", директору по научным исследованиям и разработкам Ширшину К.В. (56) Список документов, цитированных в отчете о поиске: RU 2237697, C1, 10.10.2004. US 2015/0118489, A1, 30.04.2015. WO 96/33230, A1, 24.10.1996. 2 6 1 6 2 9 8 (57) Формула изобретения Полиамидомочевинные производные димеризованной жирной кислоты , где R - или HN(CH2)6NH; R U R' - n=1 Стр.: 1 C 1 C 1 (54) ПОЛИАМИДОМОЧЕВИННЫЕ ПРОИЗВОДНЫЕ ДИМЕРИЗОВАННОЙ ЖИРНОЙ КИСЛОТЫ 2 6 1 6 2 9 8 (73) Патентообладатель(и): Федеральное государственное унитарное предприятие "Научно-исследовательский институт химии и технологии полимеров имени академика В.А. Каргина с опытным заводом" (ФГУП "НИИ полимеров") (RU) Приоритет(ы): (22) Дата подачи заявки: 16.03.2016 R U 14.04.2017 (72) Автор(ы): Фомина Евгения Валерьевна (RU), Червякова Галина Николаевна (RU), Фомин Валерий Анатольевич (RU), Кобякова Надежда Ксенофонтовна (RU)

УЛУЧШЕННЫЙ СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ НИТРОИЗОМОЧЕВИНЫ

... 1. Способ получения производных нитроизомочевины, представленных следующей общей формулой (3), в котором представленные следующей общей формулой (1) производные нитроизомочевины и представленные следующей общей формулой (2) амины или их соли, взаимодействуют в присутствии каталитического количества гидрокарбоната, ! ! где, в формуле, R1 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода или бензильную группу, ! ! где, в формуле, R2 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода; и R3 представляет собой атом водорода или алкильную группу, содержащую от 1 до 4 атомов углерода, ! ! где, в формуле, R1 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода или бензильную группу; R2 представляет собой алкильную группу, содержащую от 1 до 4 атомов углерода; и R3 представляет собой атом водорода или алкильную группу, содержащую от 1 до 4 атомов углерода. ! 2. Способ получения производных нитроизомочевины по п.1, в котором в качестве ...

(ГЕТЕРО)АРИЛЦИКЛОПРОПИЛАМИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LSD1

... 1. Соединение формулы Iв которой:А обозначает арил или гетероарил, где указанный арил или указанный гетероарил необязательно замещен одним или большим количеством R;В обозначает водород, Rили -L-E;Е обозначает арил или гетероарил, где указанный арил или указанный гетероарил необязательно замещен одним или большим количеством R;L обозначает связь, -O-, -NH-, -N(C-C-алкил)-, C-C-алкилен или гетеро-C-C-алкилен;D обозначает циклоалкильную группу, содержащую от 4 до 7 атомов С, где указанная циклоалкильная группа содержит 1 или 2 заместителя Rи дополнительно необязательно замещена одним или большим количеством Rи где циклоалкильная группа необязательно:(a) сконденсирована с фенильным или 5- или 6-членным ароматическим гетероциклическим кольцом, содержащим от 1 до 3 гетероатомов, независимо выбранных из группы, включающей N, О и S, где указанное конденсированное фенильное или указанное конденсированное ароматическое гетероциклическое кольцо необязательно замещено одним или большим количеством ...

СМЕСИ ДЛЯ ИСПОЛЬЗОВАНИЯ В ОБЛАСТИ МОДИФИКАЦИИ РЕОЛОГИЧЕСКИХ СВОЙСТВ

... 1. Композиция, способная к отверждению при температурах в интервале (Tотв) от 60 до 250°C, указанная композиция содержит i) связующий агент и ii) смесь для использования в качестве агента, контролирующего образование натеков (SCA), в указанной композиции, которая содержит (a) стимулирующий тиксотропность продукт полимочевины в виде макрочастиц, имеющий температуру плавления (Tпл1), по крайней мере, на 10°C ниже температуры отверждения (Tотв), тем самым удовлетворяя требованию Tпл1<(Tотв-10°C); и (b) второй стимулирующий тиксотропность компонент в виде макрочастиц, имеющий температуру плавления (Tпл2), такую, что он сохраняет свою дисперсную природу при температурах, по крайней мере, вплоть до температуры отверждения (Tотв). 2. Композиция по п.1, способная к отверждению при температурах (Tотв), превышающих 90°C и более предпочтительно превышающих 120°C. 3. Композиция по п.1 или 2, способная к отверждению при температурах (Tотв), находящихся между 120 и 150°C. 4. Композиция по п.1, у которой ...

Verfahren zur N-Alkylierung von Harnstoffen.

Metal-catalysed carboxymethylation in the presence of a promoter

ARYLOXYCYCLOALKENYL AND ARYLOXYIMINOCYCLOALKENYLHYDROXYUREAS AS 5-LIPOXYGENASE INHIBITORS

The present invention provides a compound of formula (I), wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C1-4 alkyl, C14 haloalkyl, C1-4 hydroxyalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C2-4 alkoxyalkoxy, C1-4 alkylthio, hydroxy, halo, cyano, amino, C1-4 alkylamino, di (C2-8) alkylamino, C2-6 alkanoylamino, carboxy, C2-6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo¢b!furyl, thienyl, benzo¢b!thienyl, pyridyl or quinolyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, halo, C1-4 alkoxy, optionally-substituted phenyl, phenoxy or phenylthio, X is C1-C4 alkylene, C2C4 alkenylene, -(CHR1)m-Q1-(CHR2)n-, -O-(CHR1)jQ2- and -(CHR1)-O-N = in which the N = moiety is attached to the cycloakene ring; and in which Q1 is O, S, SO, SO2, NR3, CH = N-O or CO, Q2 is O, S, SO, SO2 or NR3, and R1, R2 and R3 are each hydrogen or C1-C4 alkyl, m and n are each an integer from 0 to 4 and j is an integer from ...

CYCLIC PEPTIDOMIMETIC COMPOUNDS AS IMMUNOMODULATORS

Preparation of N-acyl amino carboxylic acids, amino carboxylic acids and their derivatives by metal-catalyzed carboxymethylation in the presence of a promoter

A process for the preparation of amino carboxylic acids, N-acyl amino carboxylic acids, or derivatives thereof by carboxymethylation of an amide, amide precursor or amide source compound in the presence of a carboxymethylation catalyst precursor and a promoter is provided. A carboxymethylation reaction mixture is formed by introducing a promoter, an amide, amide precursor or amide source compound, carbon monoxide, hydrogen, an aldehyde or aldehyde source compound, and a carboxymethylation catalyst precursor into a carboxymethylation reaction zone. In a preferred embodiment, the promoter is a supported noble metal promoter. In another preferred embodiment, the amide compound and aldehyde are selected to yield an N-acyl amino carboxylic acid which is readily converted to N-phosphonomethyl)glycine, or a salt or ester thereof.

N-АЛКОКСИКАРБОНИЛАМИНОЭТИЛ-N'-АРИЛМОЧЕВИНЫ, ПРОЯВЛЯЮЩИЕ РОСТ-РЕГУЛИРУЮЩУЮ АКТИВНОСТЬ

Изобретение относится к способу получения N-алкоксикарбониламиноэтил-N'-арилмочевин общей формулы I, где R=втор-СH, R=Н, R=H, R=СН(Ia), R=втор-СH, R=СН, R=H, R=H (Iб), R=изо-СH, R=СН, R=H, R=CH(Iв), R=н-CH, R=CH, R=H, R=H (Iг), R=изо-СН, R=H, R=H, R=CH(Iд), R=изо-СН, R=H, R=H, R=COOCH(Ie), R=втор-СH, R=CH, R=H, R=CH(Iж), которые могут найти применение в сельском хозяйстве для повышения устойчивости растений к неблагоприятным факторам окружающей среды. Способ включает взаимодействие соответствующих ароматических изоцианатов с алкиловыми эфирами β-аминоэтилкарбаминовой кислоты в инертном растворителе при комнатной температуре с последующим выделением целевых соединений формулы I известными приемами. Изобретение относится также к N-алкоксикарбониламиноэтил-N'-арилмочевинам общей формулы I, где R=втор-СH, R=Н, R=H, R=СН(Ia), R=втор-СH, R=СН, R=H, R=H (Iб), R=изо-CH, R=СН, R=H, R=CH(Iв), R=н-СН, R=СН, R=H, R=H (Iг), R=изо-CH, R=H, R=H, R=CH(Iд), R=втор-СH, R=CH, R=H, R=CH(Iж), которые могут ...

АРИЛОКСИЦИКЛОАЛКЕНИЛ- И АРИЛОКСИИМИНОЦИКЛОАЛКЕНИЛГИДРОКСИМОЧЕВИНЫ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ИНГИБИРУЮЩАЯ 5-ЛИПОКСИГЕНАЗУ

Настоящее изобретение относится к новым производным арилоксициклоалкенил- и арилоксииминоциклоалкенилгидроксимочевинам. Соединения данного изобретения ингибируют действие фермента 5-липоксигеназы и полезны для профилактики, лечения или облегчения течения заболеваний, связанных с воспалительными процессами, таких, как воспаление кишечника и ревматоидный артрит, аллергия и сердечно-сосудистые заболевания у млекопитающего субъекта, например у человека. Данное изобретение относится также к фармацевтическим композициям, включающим эти соединения. 2 с. и 5 з.п. ф-лы, 1 табл.

СОЕДИНЕНИЯ, ЯВЛЯЮЩИЕСЯ ИНГИБИТОРАМИ ГЛИКОГЕНФОСФОРИЛАЗЫ, И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ

... 1. Соединение формулы 1:его фармацевтически приемлемая соль, сольват или физиологически функциональное производное,где А представляет собой C(=O)NQQили С(=O)ОН;Qи Qконденсированы вместе;Qвыбран из группы, состоящей из (1) 5- или 6-членного ароматического кольца, (2) 5- или 6-членного циклоалкильного кольца, (3) 5- или 6-членного гетероароматического кольца, имеющего по меньшей мере один гетероатом, выбранный из группы, состоящей из азота, кислорода или серы, и (4) 4-8-членного гетероциклического кольца, имеющего по меньшей мере один гетероатом, выбранный из группы, состоящей из азота, кислорода или серы; и q равно 0 или 1;Qвыбран из группы, состоящей из (1) 5- или 6-членного ароматического кольца и (2) 5- или 6-членного гетероароматического кольца, имеющего по меньшей мере один гетероатом, выбранный из группы, состоящей из азота, кислорода или серы;каждый из Rи Rнезависимо выбран из группы, состоящей из водорода, Салкила, галогено, алкокси, моноалкиламино и диалкиламино;Rпредставляет собой ...

СПОСОБ И УСТРОЙСТВО ДЛЯ ПОЛУЧЕНИЯ МОЧЕВИННОЙ КОНСИСТЕНТНОЙ СМАЗКИ

... 1. Способ получения мочевиновой консистентной смазки, который включает в себя (а) введение первого исходного компонента в первую зону подачи; (b) введение второго исходного компонента во вторую зону подачи; (с) первое взаимодействие-смешивание в первой зоне взаимодействия-смешивания; и (d) охлаждение-смешивание в зоне охлаждения-смешивания, и который осуществляют в экструдере, включающем в себя указанные зоны, которые расположены в последовательности (а), (b), (с), (d). ! 2. Способ по п.1, дополнительно включающий подачу масла в зону подачи масла. ! 3. Способ по п.1, дополнительно включающий смешивание в зоне смешивания. ! 4. Способ по п.1, в котором мочевиновая консистентная смазка содержит тетрамочевиновую консистентную смазку. ! 5. Способ получения мочевиновой консистентной смазки, который включает в себя (а) введение первого исходного компонента в первую зону подачи; (b) введение второго исходного компонента во вторую зону подачи; (с) первое взаимодействие-смешивание в первой зоне взаимодействия-смешивания ...

VERFAHREN ZUR HERSTELLUNG VON GUANIDINDERIVATEN, ZWISCHENPRODUKTE DAFÜR UND IHRE HERSTELLUNG

SUBSTITUTED 1,3- DIAMINOPROPANES

N min -Acyl-N-alkyl-1,3-diaminopropanes of formula R<1>CONH(CH2)3NHR<2> (where R<1> is R- or RNH where R is a substituted or unsubstituted hydrocarbon group and R<2> is alkyl) are prepared by selectively acylating N-alkyl-1,3-diaminopropanes. In the process a N-alkyl-1,3-aminopropane is reacted with an aldehyde to form a hexahydropyrimidine, the hexahydropyrimidine is acylated and the acylated hexahydropyrimidine is then hydrolysed to give the product.

SUBSTITUTED 1,3-DIAMINOPROPANES

PROCESS FOR PRODUCING GUANIDINE DERIVATIVES, INTERMEDIATES THEREFOR AND THEIR PRODUCTION

A process for producing the compound (I) or a salt thereof having excellent pesticidal activity as shown in the above schema (i).

PROCESS FOR PRODUCING GUANIDINE DERIVATIVES, INTERMEDIATES THEREFOR AND THEIR PRODUCTION

A process for producing the compound (I) or a salt thereof having excellent pesticidal activity as shown in the above schema (i).

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

Process for the preparation of urethanes

Urethanes are prepared by oxidative carbonylation of at least one amino compound in the presence of carbon monoxide, oxygen and organic, at least one hydroxyl-group-carrying compound. The carbonylation is carried out in the absence of halogen-containing promoters. The carbonylation is also carried out in the presence of a metal complex catalyst which contains neutral bidentate N-chelate ligands of the (N~N) type, two monoanionic N,O-chelate ligands of the general type (N~O)- or tetradentate dianionic chelate ligands (O~N~N~O)2-.

Polyurea Compound

A polyurea compound obtainable by reacting one or more polyisocyanates with one or more non-chiral mono-amines (I) and one or more chiral mono-amines (II) and co-precipitating the reaction products to form the polyurea compound, wherein 2-98 mole % of the mono-amines in the polyurea compound are chiral mono-amines. The invention also relates to the use of said polyurea compound as a rheology modification agent, in particular as sag control agent (SCA) in coating compositions. The invention further relates to sag control agent compositions, coating compositions and coatings comprising the polyurea compound as sag control agent.

Process for the preparation of aminoacid derivatives

СПОСОБ СИНТЕЗА(Z)-3-[2-БУТОКСИ-3'-(3-ГЕПТИЛ-1-МЕТИЛУРЕИДО)БИФЕНИЛ-4-ИЛ]-2-МЕТОКСИАКРИЛОВОЙ КИСЛОТЫ

Настоящее изобретение относится к новому способу синтеза (Z)-3-[2-бутокси-3'-(3-гептил-1-метилуреидо)бифенил-4-ил]-2-метоксиакриловой кислоты формулы (I) и промежуточным соединениям (XII), (XIII) и (XIV). Предложенный способ заключается во взаимодействии сульфоната формулы (XII), где Rозначает метил, трифторметил, фенил или толил, с 3-гептил-1-метил-1-[3-(4,4,5,5 -тетраметил [1,3,2] диоксаборолан-2-ил)фенил] мочевиной формулы (IIIb) или с соответствующей бороновой кислотой формулы (IIIa). Технический результат заключается в упрощении синтеза за счет сокращения стадий. 4 н. и 4 з.п. ф-лы, 1 пр., 2 ил.

АЛЬДИМИНСОДЕРЖАЩИЕ СОЕДИНЕНИЯ

... 1. Альдиминсодержащее соединение формулы (I): ! ! где m означает целое число от 1 до 4, ! р означает целое число от 1 до 6, ! q означает целое число от 0 до 5, ! с тем соответствием, что р+q = 2-6; ! и причем ! R1 либо означает одновалентный углеводородный остаток с 6-30 атомами углерода, который возможно включает, по меньшей мере, один гетероатом, в особенности, в форме кислорода простого эфира, ! либо означает заместитель формулы (II): ! ! где R6 означает двухвалентный углеводородный остаток с 2-20 атомами углерода, который возможно включает, по меньшей мере, один гетероатом, в особенности, в форме кислорода простого эфира, и ! R7 означает одновалентный углеводородный остаток с 1-20 атомами углерода; ! и где R2 и R3 либо, независимо друг от друга, каждый, означают одновалентный углеводородный остаток с 1-12 атомами углерода, либо вместе образуют двухвалентный углеводородный остаток с 4-20 атомами углерода, который является частью возможно замещенного карбоцикла с 5-8, предпочтительно ...

ПОЛИМОЧЕВИННОЕ СОЕДИНЕНИЕ

... 1. Полимочевинное соединение, которое может быть получено реакцией одного или нескольких полиизоцианатов с одним или несколькими нехиральными моноаминами (I) и одним или несколькими хиральными моноаминами (II), и совместно выпадающие в осадок продукты реакции с образованием полимочевинного соединения, где 2-98 мол.% моноаминов в полимочевинном соединении представляют собой хиральные моноамины. 2. Полимочевинное соединение по п.1, которое может быть получено реакцией одного или нескольких полиизоцианатов со смесью нехиральных моноаминов формулы (I) и хиральных моноаминов формулы (II), где смесь включает в себя 2-98 мол.% хирального моноамина II, где каждый из R1-R3 является независимо выбранный из группы, состоящей из линейного или разветвленного, замещенного или незамещенного, насыщенного или ненасыщенного гидрокарбила или гетероатомсодержащей группы, где R2 и R3каждого хирального моноамина II являются различными, так что атом углерода в моноамине II является хиральным центром. 3. Полимочевинное ...

(hetero)aryl cyclopropylamine compounds as LSD1 inhibitors

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

N-PHENYL-N'-ACYLISOTHIOUREAS

N-pheny1-N'-acylisothioureas The invention relates to novel substituted N-phenyl-N'-acylisothio-ureas of the formula wherein R1 is C1-C5alkyl. R2 is hydrogen or C1-C5alkyl, R3 is hydrogen, halogen, C1-C5alkyl, phenoxy or phenoxy which is substituted by 1 or 2 identical or different members selected from the group consisting of halogen atoms, C1-C5alkyl or trifluoromethyl radicals, R4 is C1-C5alkyl, allyl or propargyl, R5 is C1-C5alkyl, C3-C6cycloalkyl, allyl or propargyl, and R6 is a radical selected from -CO-R7, -CO-CO-R8, -SO2-R7 or -CO-OR7, wherein R7 is C1-C5alkyl, phenyl or phenyl which is substituted by 1 or 2 halogen atoms or methyl groups, and R8 is C1-C10alkoxy or C1-C5dialkylamino. The invention further relates to the preparation of these compounds and to compositions containing them for use in pest control, in particular for controlling plants and animals which are atacked by insects. The novel compounds are in particular very effective against plant destructive feeding ...

SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING THESE, METHODOF PRODUCTION AND USE

La présente invention concerne notamment de nouveaux composés chimiques, particulièrement des pyrazoles substitués, les compositions les contenant, e t leur utilisation comme médicaments.

METHOD FOR THE SYNTHESIS OF (Z)-3-[2-BUTOXY-3'-(3-HEPTYL-1-METHYL-UREIDO)-BIPHENYL-4-YL]-2-METHOXY-ACRYLIC ACID

L'invention concerne un précède de synthèse de I'acide (Z)-3-[2-butoxy-3' -(3-heptyl-1 - methyl-ureido)-biphenyl-4-yl]-2-methoxy-acrylique de formule (I), et également Ie précède de synthèse des intermédiares reactionnels de f ormule generale (XII) ainsi que lesdits composés lorsque R2 est choisi parmi les radicaux méthyle, trifluoromethyl, phenyl et 4-tolyl formule (XII) ...

CYCLIC PEPTIDOMIMETIC COMPOUNDS AS IMMUNOMODULATORS

The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

USE OF MONOCHLOROUREA TO TREAT INDUSTRIAL WATERS

The present invention comprises a method for controlling (e.g. inhibiting) or killing microorganisms in an aqueous environment. The method includes the addition of an effective amount of monochlorourea or modified monochlorourea to an aqueous solution. This aqueous solution may be a cooling water system, a recreational water system, a water treatment facility, or any circulating water system (i.e. a papermaking facility). A method of producing monochlorourea or modified monochlorourea is also disclosed.

PREPARATION OF MONOBASIC PHOSPHATE IONOPHORES

The present invention relates to the synthesis of lipophilic or immobilized monobasic phosphate (H2PO4) ionophores (7, 8a, 8b and 11) to be used as ion recognition molecules for monobasic phosphate (H2PO4") in the cocktail preparation of hydrophobic polymer membranes in ion selective electrode (ISE) or ion-sensitive field effect transistor (ISFET) chemical sensors for detection of monobasic phosphate (H2PO4 ) ionic species in soil, synthetic media, hydrophonic liquid, tree sap, ground water and rivers.

METHOD FOR PRODUCING A COMPOUND WITH AT LEAST ONE AT LEAST MONOSUBSTITUTED AMINO GROUP

Verfahren zur Herstellung einer Verbindung mit mindestens einer zumindest einfach substituierten Aminogruppe

Die Erfindung betrifft ein Verfahren zur Herstellung einer Verbindung mit mindestens einer zumindest einfach substituierten Aminogruppe. Erfindungsgemäß wird dazu eine mindestens eine Aminogruppe tragende Ausgangssubstanz mit einem Alkohol in einer Reaktionsmischung in Gegenwart von Ammoniak umgesetzt.

SUBSTITUTED 1,3-DIAMINOPROPANES

Supports for solid phase synthesis

Epoxidation of glycerol and derivatives therefrom

A method producing a surfactant from glycerol by converting glycerol, in a first step, to glycidol, polymerizing glycidol to an aliphatic alcohol and finally substituting a hydroxyl group with a substitute anion.

(Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors

A NOVEL KCNQ POTASSIUM CHANNEL AGONIST, THE PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound with a structure represented by general formula I or a pharmaceutically acceptable salt thereof, a preparation method for the compound or the salt, and a use of the compound or the pharmaceutically acceptable salt thereof in the preparation of medicaments for treating nervous system diseases, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke or neurodegenerative diseases. Compared with Retigabine, the compound of the present invention has better brain tissue absorption. Moreover, the compound provided by the present invention not only has greatly improved efficacy, but also has far fewer neurological side effects than Retigabine, and therefore has a wider safe window.

Process for preparing polyisocyanates containing biuret groups

The present invention relates to a process for preparing polyisocyanates containing biuret groups from di- or polyisocyanates with diamines.

Method for extracting citrulline from watermelon

The present invention relates to the technical field of natural substance extraction. Disclosed is a method for extracting Citrulline from a watermelon. The method for extracting Citrulline from a watermelon in the present invention comprises Raw material pretreatment, ultrasound-enzymatic hydrolysis assisted solvent leaching, and purification steps. The purification step comprises microbial fermentation, ion-exchange resin purification, macroporous adsorption resin discoloration, and crystallization and recrystallization. The method for extracting Citrulline in the present invention is simple, requires a mild condition, and has a good extraction effect on Citrulline. The purity of Citrulline after purification is more than 90%. In addition, the Citrulline extracted by the method in the present invention meets the related health requirements and product quality standards, can be applied to food and health food industries as a raw material, and has natural security advantages.

Substituted ureas and methods of making and using same

The invention relates to substituted ureas, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.

IMPROVED PROCESS FOR PRODUCING NITROISOUREA DERIVATIVES

Disclosed is an improved process for producing nitroisourea derivatives which is necessary for producing nitroguanidine derivatives having an insecticidal activity. Specifically disclosed is a process for producing nitroisourea derivatives represented by the following general formula (3), which is characterized in that nitroisourea derivatives represented by the following general formula (1) and amines represented by the following general formula (2) or a salt thereof are reacted in the presence of a catalytic amount of a hydrogen carbonate, (see formula 1) (see formula 2) (see formula 3) ...

Ureido-containing neuraminidase inhibitor and medical application thereof

SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING THEM, METHOD OF MANUFACTURE AND USE

La présente invention concerne notamment de nouveaux composés chimiques, particulièrement des pyrazoles substitués, les compositions les contenant, et leur utilisation comme médicaments.

METHOD FOR OBTAINING SYMMETRICAL N,N'-DISUBSTITUTED UREA

The present invention relates to a method for obtaining symmetrical N,N'-disubstituted urea, comprising the step of reacting a reaction mixture comprising a primary amine and phosgene corresponding to the substituents of the urea in an at least two-phase system comprising an aqueous phase, wherein the temperature during the reaction is higher than 20ºC, and the pH of at least the aqueous phase is higher than 7.

METHOD FOR PRODUCING A COMPOUND WITH AT LEAST ONE AT LEAST MONOSUBSTITUTED AMINO GROUP

The invention relates to a method for producing at least one compound having at least one at least monosubstituted amino group. According to the invention, a starting substance supporting at least one amino group is reacted with an alcohol in a reaction mixture in the presence of ammoniac.

A novel KCNQ potassium channel agonist, the preparation method therefor and use thereof

The present invention provides a compound with a structure represented by general formula I or a pharmaceutically acceptable salt thereof, a preparation method for the compound or the salt, and a use of the compound or the pharmaceutically acceptable salt thereof in the preparation of medicaments for treating nervous system diseases, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke or neurodegenerative diseases. Compared with Retigabine, the compound of the present invention has better brain tissue absorption. Moreover, the compound provided by the present invention not only has greatly improved efficacy, but also has far fewer neurological side effects than Retigabine, and therefore has a wider safe window.

Epoxidation of glycerol and derivatives therefrom

A method producing a surfactant from glycerol by converting glycerol, in a first step, to glycidol, polymerizing glycidol to an aliphatic alcohol and finally substituting a hydroxyl group with a substitute anion.

METHOD FOR PREPARING BROMOUREA

The invention provides a process for manufacturing biocidal compositions containing bromourea derivatives, including the reaction of salts or adducts of the urea derivatives with an oxidizer. 1. A method for manufacturing a bromourea derivative , comprising reacting a salt or adduct of a urea derivative of the general structure A-U , where A stands for an acid and U stands for the urea derivative , with an oxidizer , while combining aqueous solutions of said urea derivative , of said acid , and of said oxidizer , wherein said urea derivative is in a molar excess over said acid , and the molar ratio of said acid to said oxidizer is at least 1.0.2. The method according to claim 1 , wherein said urea derivative is in at least four fold molar excess over said acid and at least ten fold excess over said oxidizer.3. The method according to claim 1 , wherein said urea derivative is in about fifteen fold molar excess over said acid claim 1 , and wherein said molar ratio of said acid to said oxidizer is at least 2.0.4. The method for manufacturing a bromourea derivative according to claim 1 , comprising reacting a salt or adduct of the general structure A-U with an oxidizer claim 1 , where A stands for HCl or HBr claim 1 , and wherein U stands for urea.5. The method according to where A stands for HCl claim 4 , comprisingi) reacting said salt or adduct with NaOCl, thereby forming chlorourea, andii) adding to said chlorourea a solution comprising NaBr, thereby obtaining a composition comprising bromourea.6. The method according to where A stands for HBr or a mixture of HBr with HCl claim 4 , comprising reacting said salt or adduct with NaOCl claim 4 , thereby forming bromourea and obtaining a composition comprising bromourea.7. The method according to claim 1 , wherein said oxidizer is selected from NaOCl claim 1 , LiOCl claim 1 , Ca(OCl) claim 1 , ClO claim 1 , ozone claim 1 , urea hydroperoxide claim 1 , hydrogen peroxide claim 1 , hydrogen peroxide precursors claim 1 , ...

PHENOXYPROPANOL DERIVATIVES AND THEIR USE IN TREATING CARDIAC AND CARDIOVASCULAR DISEASES

A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: 2. The compound as claimed in wherein Ris selected from unsubstituted and substituted Ccycloalkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , Calkyl claim 1 , Caryl-Calkyl claim 1 , Calkoxy-Caryl-Calkyl.3. The compound as claimed in wherein Xis selected from CO claim 1 , CS claim 1 , SOand a single bond.4. The compound as claimed in wherein Rand Rare selected from ROZO as hereinbefore defined claim 1 , m- claim 1 ,p-(OCH)or o- claim 1 , m- or p-OH claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , NH claim 1 , R claim 1 , OR claim 1 , or CFor a combination thereof.12. A process for the preparation of a compound of formula I-0 or subformulae as defined in .14. A composition comprising a therapeutically effective amount of a compound of formula I-0 or subformulae or its pharmaceutically acceptable salt and physiologically hydrolysable derivative as defined in in association with one or more pharmaceutical carriers or diluents.15. The use of a compound of formula I-0 or subformulae or pharmaceutically acceptable salt or composition as defined in in the prevention or treatment of a condition selected from ischaemic heart disease claim 1 , hypertension and heart failure claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD.16. A method of treating a condition selected from ischaemic heart disease (also known as myocardial infarction or angina) claim 1 , hypertension and heart failure claim 1 , restenosis and cardiomyopathy claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD claim 1 , said method comprising administering to a subject in need thereof claim 1 , a compound of formula I-0 or subformulae or pharmaceutically acceptable salt or composition thereof as defined in in an amount sufficient to treat the condition.17. A method of ...

method for preparing 2-(N-substituted)-amino-benzimidazole derivatives

A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.

ENANTIOMERICALLY PURE BINAPHTHOL DERIVATIVES AND METHOD FOR PREPARING THE SAME

The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2′-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost. [formula 6] 7. The method for preparing according to claim 6 , wherein the base is an organic base which is triethylamine (TEA) or tetramethylethylenediamine (TMEDA) claim 6 , or an inorganic base selected from the group consisting of NaH claim 6 , NaOH claim 6 , KOH and KCO.8. The method for preparing according to claim 6 , wherein the organic solvent is selected from the group consisting of N claim 6 ,N-dimethylformamide claim 6 , dimethylsulfoxide claim 6 , N-methylpyrrolidone and tetrahydrofuran.12. The method for preparing according to claim 7 , wherein the organic solvent is selected from the group consisting of N claim 7 ,N-dimethylformamide claim 7 , dimethylsulfoxide claim 7 , N-methylpyrrolidone and tetrahydrofuran. The present invention relates to novel compounds used as an important intermediate in the method for preparing the compound of a 2,2′-binaphthol-3-aldehyde derivative and a method for preparing the same.Compounds where the hydrogen of the 2′ hydroxyl group in 2,2′-binaphthol-3-aldehyde is selectively substituted are used for various uses. Among such compounds, the compound of the following formula 6, which is very useful for separating chiral amino alcohols or amino acids into their respective optical isomers by recognizing their chirality through an imine bond or for converting L-amino acid into D-amino acid or D-amino acid into L-amino acid, has been developed by the inventors of the present invention and patented (Korean Patent No. 0661280). ...

ELECTROCHEMICAL GENERATION OF CHLORINATED UREA DERIVATIVES

Method of single step electrochemical generation of chlorinated urea, chlorinated dimethylurea and other chlorourea derivatives is disclosed. The chlorinated species are generated in situ and upon demand and can be used for microbial control in industrial water treatment. 1. A method of generation of chlorinated urea or chlorinated urea derivatives comprising:i) charging an electrochemical cell with a chloride solution containing a) a chloride source; b) urea, urea derivative, or combinations thereof; and c) acid;ii) electrochemically generating at least one active halogen donor species;iii) wherein the at least one active halogen donor species reacts with urea, urea derivative, or combinations thereof, in the solution to produce a chlorinated urea or a chlorinated urea derivative in situ.2. The method of claim 1 , wherein the chloride source is a soluble inorganic chloride3. The method of claim 2 , wherein the chloride source is selected from the group consisting of sodium chloride claim 2 , potassium chloride claim 2 , lithium chloride claim 2 , hydrochloric acid and combinations thereof.4. The method of claim 1 , wherein the urea derivative comprises N claim 1 ,N′-dimethylurea.5. The method of claim 3 , where in the acid comprises phosphoric acid.6. The method of claim 1 , wherein the chlorinated urea derivative comprises N-chloro-N claim 1 ,N′-dimethylurea.7. The method of claim 1 , wherein the pH of the solution in iii) is less than or equal to 7.8. The method of claim 1 , wherein the acid comprises phosphoric acid.9. The method of claim 1 , wherein the pH of the initial chloride solution containing dimethylurea claim 1 , soluble chloride claim 1 , and acid prior to the electrolysis of step ii) is from about 1 to 7.10. The method of claim 9 , wherein the pH of the initial chloride solution is from about 1 to 3.11. The method of claim 4 , wherein the pH of the final solution after the electrolysis containing N-chloro-N claim 4 ,N′-dimethylurea derivative is from ...

METHOD FOR CONVERTING MONOISOCYANATES TO UREAS

Organic isocyanates are converted to ureas by heating in the presence of certain cobalt, magnesium, chromium and lanthanide series organometallic catalysts. The process requires no water or other reactants. The process is particularly useful for removing small quantities of monoisocyanates from a solvent stream recovered from a polyisocyanate manufacturing process. The urea compounds in some instances can be recycled back into the polyisocyanate manufacturing process and reacted with polyisocyanate compounds to form biurets. 1. A method for converting an organic isocyanate comprising a phenyl isocyanate to one or more urea compounds in the presence of a non-polar organic solvent , comprising reacting a solution of the organic isocyanate in a liquid nonpolar solvent in the presence of at least 0.025 wt.-% of a organometallic catalyst , based on the weight of the organic isocyanate , wherein the organometallic catalyst includes at least one metal ion bonded to at least one organic ligand and the metal ion is selected from one or more of Co(II) , Mg(II) , Y(III) , Cr(III) and a lanthanide series metal ion in the 3+ oxidation state , to convert at least a portion of the organic isocyanate to the one or more urea compounds.2. The method of wherein the metal ion is Co(II) or Mg(II).3. The method of wherein at least one organic ligand is an arene ligand.4. The method of wherein the arene ligand is cyclopentadienyl or methylcyclopentadienyl.5. The method of wherein the metallic catalyst is one or more of bis(cyclopentadienyl) Co(II) claim 1 , bis(cyclopentadienyl) Mg(II) claim 1 , bis(cyclopentadienyl) Cr(II) claim 1 , tris(cyclopentadienyl) Gd(III) claim 1 , tris(cyclopentadienyl) Y(III) claim 1 , tris(cyclopentadienyl) La(III) claim 1 , tris(cyclopentadienyl Ru(III) claim 1 , bis(methylcyclopentadienyl) Co (II) claim 1 , bis(methylcyclopentadienyl) Mg(II) claim 1 , bis(methylcyclopentadienyl) Cr(II) claim 1 , tris (methylcyclopentadienyl) Gd(III) claim 1 , tris ( ...

UREA DERIVATIVES AND THEIR USE AS FATTY-ACID BINDING PROTEIN (FABP) INHIBITORS

The invention provides novel compounds having the general formula (I) 2. A compound according to claim 1 , wherein Rand Rtogether with the carbon they are attached to form a cyclopropyl claim 1 , a cyclobutyl or a cyclopentyl.3. A compound according to claim 1 , wherein Rand Rtogether with the carbon they are attached to form a cyclopropyl or a cyclopentyl.4. A compound according to claim 1 , wherein Ris H or alkyl.5. A compound according to claim 1 , wherein Ris H.6. A compound according to claim 1 , wherein Ris H.7. A compound according to claim 1 , wherein W is a bond.8. A compound according to claim 1 , wherein A is phenyl substituted with R claim 1 , Rand R.9. A compound according to claim 1 , wherein A is phenyl claim 1 , trifluoromethylphenyl claim 1 , chlorophenyl claim 1 , dichlorophenyl or chlorofluorophenyl.10. A compound according to claim 1 , wherein A is chlorophenyl or chlorofluorophenyl.11. A compound according to claim 1 , wherein B is phenyl substituted with R claim 1 , Rand R.12. A compound according to claim 1 , wherein B is phenyl or fluorophenyl.13. A compound according to claim 1 , wherein R claim 1 , Rand Rare independently selected from H claim 1 , haloalkyl and halogen.14. A compound according to claim 1 , wherein R claim 1 , Rand Rare independently selected from H and halogen.15. A compound according to claim 1 , wherein R claim 1 , Rand Rare independently selected from H and halogen.16. A compound according to claim 1 , selected from the group consisting of:1-(3-(biphenyl-2-yl)-1-methylureido)cyclopropanecarboxylic acid;1-(3-(4-chlorobiphenyl-2-yl)ureido)cyclopentanecarboxylic acid;1-(3-(4-chlorobiphenyl-2-yl)ureido)cyclopropanecarboxylic acid;1-(3-(4-chlorobiphenyl-2-yl)ureido)cyclobutanecarboxylic acid;1-(3-(4-chloro-4′-fluorobiphenyl-2-yl)ureido)cyclopropanecarboxylic acid;1-(3-(4-chloro-4′-fluorobiphenyl-2-yl)ureido)cyclopentanecarboxylic acid;1-(3-(4-chloro-5-fluorobiphenyl-2-yl)ureido)cyclopropanecarboxylic acid;1-(3-(5- ...

Synthesis of Carbamate or Urea Compounds

The invention pertains to the synthesis of carbamate and urea compounds. In particular the invention is directed to the synthesis of carbamate and urea compounds which may be used in the production of compounds that are used to stabilize nitrocellulose. The method of the invention comprises preparing a carbamate or urea derivative comprising reacting an amine and a carbonate or carbamate in the presence of an ionic liquid. 2. Method according to claim 1 , wherein the catalyst comprises an ionic liquid.3. Method according to claim 2 , wherein the ionic liquid comprises a cation and an anion and wherein the cation is a N claim 2 ,N-dialkyl imidazolium claim 2 , preferably a 1-alkyl-3-methylimidazolium claim 2 , preferably 1-ethyl-3-methylimidazolium or 1-butyl-3-methylimidazolium (BMIm) and/or the anion is selected from the group consisting of hydroxide claim 2 , chloride claim 2 , bromide claim 2 , iodate claim 2 , acetate claim 2 , hexafluorophosphate claim 2 , tetrafluoroborate and combinations thereof claim 2 , preferably the anion is a hydroxide or a chloride.4. Method according to claim 1 , wherein the catalyst comprises a non-nucleophilic base claim 1 , preferably a superbase claim 1 , more preferably a superbase selected from the group consisting of amidines claim 1 , phosphazenes and guanidines claim 1 , even more preferably amidines claim 1 , most preferably 1 claim 1 ,8-diazabicyclo[5.4.0]undec-7-ene (DBU).5. Method according to claim 1 , wherein Aris a phenyl claim 1 , optionally substituted with one or more halide claim 1 , alkoxy claim 1 , nitro claim 1 , sulfonate claim 1 , ester claim 1 , amide claim 1 , carboxylate and Aris Aror a phenyl and is optionally substituted with one or more halide claim 1 , alkoxy claim 1 , nitro claim 1 , sulfonate claim 1 , ester claim 1 , amide claim 1 , carboxylate claim 1 , preferably both Arand Arare phenyl such that the amine according to formula II is diphenylamine.6. Method according to claim 1 , wherein X is a C- ...

THERMO-THICKENING COMPOUNDS FOR NON-POLAR LIQUID

A bis-urea compound of general formula (IV): 115-. (canceled)18. The method according to claim 17 , wherein in the compound of formula (IVbis) claim 17 , Rand Rare both H.19. The method according to claim 16 , wherein said composition is a non-polar liquid.20. The method according to claim 16 , wherein thermo-thickening is performed at a temperature ranging from 5° C. to 100° C.21. The method according to claim 16 , for further improving the cold flow property of a non-polar liquid.23. The compound according to claim 22 , wherein n is equal to 0 (i.e. compounds having formula (IV bis)).24. The compound according to claim 23 , wherein Z claim 23 , Z′ claim 23 , Zand Z′ represent O atoms.25. The compound according to claim 24 , selected from:(2S,2′S)-dihexyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-diheptyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-dioctyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-dioctyl 2,2′-((((4,6-dimethyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-dioctyl 2,2′-((((4,6-dichloro-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-dinonyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-dinonyl 2,2′-((((4,6-dimethyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-didecyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-diundecyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-didodecyl 2,2′-((((4-methyl-1,3-phenylene)bis(azanediyl))bis(carbonyl))bis(azanediyl))bis(3-phenylpropanoate);(2S,2′S)-didodecyl 2,2′-((((4,6-dimethyl-1,3-phenylene)bis( ...

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: 19-. (canceled)11. The process of claim 10 , wherein the second suitable solvent is chloroform claim 10 , dichloromethane claim 10 , nitromethane claim 10 , dimethylforamide claim 10 , diethyl ether claim 10 , tetrahydrofuran claim 10 , dioxane claim 10 , dichloroethane claim 10 , or hexane.12. The process of claim 10 , wherein step (b) is carried out at room temperature.13. The process of claim 10 , wherein step (b) is carried out at a temperature of 50-140° C.14. The process of claim 10 , wherein the compound is maintained in the second suitable solvent for 10-50 hours.15. The process of claim 10 , wherein A is a phenyl or pyridine.16. The process of claim 10 , wherein A is a furan claim 10 , thiophene claim 10 , pyrrole claim 10 , thiazole claim 10 , imidazole claim 10 , pyrazole claim 10 , isooxazole claim 10 , isothiazole claim 10 , naphthalene claim 10 , anthracene claim 10 , pyrimidine claim 10 , pyrazine claim 10 , pyridazine claim 10 , indole claim 10 , indoline claim 10 , benzofuran claim 10 , benzothiophene claim 10 , or quinolone.2037-. (canceled) This application claims priority of U.S. Provisional Application Nos. 62/192,789, filed Jul. 15, 2015; 62/192,462, filed Jul. 14, 2015; 62/063,246, filed Oct. 13, 2014; and 62/062,508, filed Oct. 10, 2014, the contents of each of which are hereby incorporated by reference.Throughout this application various publications are referenced. The disclosures of these documents in their entireties are hereby incorporated by reference into this application in order to more fully describe the state of the art to which this invention pertains.Fluorine atoms are often introduced into organic molecules to enhance their pharmacological properties such as solubility, metabolic and oxidative stability, lipophilicity, and bioavailability. Among the fluorine containing functional groups, ...

ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE

The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose. 1. A method of carrying out an organic reaction in a solvent containing at least 90% by weight , based on the total weight of the solvent , of water , which method comprises reacting the reagents in said solvent in the presence of a cellulose derivative as a surfactant which is selected from the group consisting of cellulose modified with one or more alkylene oxides or other hydroxyalkyl precursors , and alkylcellulose;where the organic reaction is not a polymerization or oligomerization reaction of olefinically unsaturated compounds; and [ a transition metal catalyzed C—C coupling reaction:', 'a transition metal catalyzed reaction involving C—N bond formation which is an Au-catalyzed cyclodehydratization of α,β-amino alcohols containing a C—C triple bond:', 'a transition metal catalyzed reaction involving C—O bond formation:', 'a transition metal catalyzed reaction involving C—S bond formation:', 'a transition metal catalyzed reaction involving C—B bond formation: or', 'a transition metal catalyzed reaction involving C-halogen bond formation; or, 'a transition metal catalyzed reaction in which a transition metal catalyst is used; where the transition metal catalyzed reaction is'}, 'a C—C coupling reaction not requiring transition metal catalysis which is selected from the group consisting of reactions of carbonyl or nitrile compounds and pericyclic reactions;, 'where the organic reaction is'}a nucleophilic substitution reaction;a reduction or an oxidation reaction; oran ester formation reaction or an ester hydrolysis reaction.2. The method as claimed in claim 1 , where the cellulose derivative has a viscosity of from 1 to 150000 mPa·s claim 1 , determined as a 2% by weight aqueous solution claim 1 , relative to the weight of water.3. The method as claimed in claim 1 , where in the cellulose ...

UREA PLANT WITH STRIPPER AND STRIPPING METHOD

A method is disclosed for stripping in a stripper a urea synthesis solution received from a urea forming process wherein ammonia and CO2 are reacted under urea forming conditions. The shell space of the stripper comprises a continuous vertical zone. 2. The method according to claim 1 , wherein said continuous vertical zone does not include baffles.3. The method according to claim 1 , wherein tubes are supported by strips having a width of less than 10 mm.4. The method according to claim 1 , wherein the continuous vertical zone has a vertical length that is at least 90% of the effective tube length.5. The method according to claim 1 , wherein the stripping is COstripping claim 1 , ammonia stripping claim 1 , or self-stripping.6. The method according to claim 1 , wherein the two circular areas both have a diameter of 0.60 m.7. A urea plant comprising a high pressure synthesis section comprising a urea reaction section claim 1 , a high pressure carbamate condenser and a stripper claim 1 , wherein the stripper is configured as vertical falling film shell-and-tube heat exchanger and comprises a tube bundle comprising tubes claim 1 , a shell claim 1 , and an upper tube sheet and lower tube sheet claim 1 , and a shell space provided in the shell between the upper and lower tube sheet claim 1 , wherein the stripper is adapted for maintaining a falling film of urea synthesis solution to be stripped in the tubes and comprises an inlet for gaseous heating fluid supplied to the shell space and an outlet for gaseous heating fluid and heating fluid condensate from the shell space claim 1 ,wherein the tube bundle has an effective tube length of 4 to 9 m, wherein the effective tube length is the length of the tube part that is in operation in contact with the heating fluid,wherein the tube bundle has an outer tube limit and a ratio of the effective tube length to the outer tube limit diameter that is 2.5 or less, wherein the outer tube limit is diameter of the circle created by ...

THIXOTROPIC AGENT FOR CURABLE COMPOSITIONS

A thixotropic agent for increasing the yield point of a curable composition, wherein the thixotropic agent includes (i) at least one urea compound from the reaction of at least one isocyanate with at least one amine and (ii) at least one polyether having blocked hydroxyl groups. The thixotropic agent is preparable in a simple manner and forms a spreadable paste which is firm at room temperature. It is particularly suitable as a constituent of moisture-curing polyurethane or SMP compositions, giving a good increase in the yield point thereof, without adversely affecting storage stability or migration characteristics. It enables phthalate-free adhesives, sealants or coatings that have surprisingly good conveyability coupled with a high yield point, and do not cause any problems with odor or fogging. 1. A thixotropic agent for increasing the yield point of a curable composition , wherein the thixotropic agent comprises (i) at least one urea compound from the reaction of at least one isocyanate with at least one amine and (ii) at least one polyether having blocked hydroxyl groups which is free of urethane groups.3. The thixotropic agent as claimed in claim 1 , wherein the thixotropic agent takes the form of a spreadable paste which is firm at room temperature.4. The thixotropic agent as claimed in claim 1 , wherein 5% to 25% by weight of urea compounds and 50% to 95% by weight of polyethers having blocked hydroxyl groups are present.5. The thixotropic agent as claimed in claim 1 , wherein the polyether having blocked hydroxyl groups has a viscosity at 20° C. in the range from 30 to 500 mPa·s claim 1 , where the viscosity is determined with a cone-plate viscometer having cone diameter 25 mm claim 1 , cone angle 1° claim 1 , cone tip-plate distance of 0.05 mm claim 1 , at a shear rate of 10 s.6. The thixotropic agent as claimed in claim 1 , wherein the polyether has an average of 1 to 3 blocked hydroxyl groups per molecule.7. The thixotropic agent as claimed in claim 1 , ...

REACTIVE AMINE CATALYSTS FOR POLYURETHANE APPLICATIONS

Tertiary amine catalysts having isocyanate reactive groups that are capable of forming thermally stable covalent bonds able to withstand temperatures up to 120° C. are disclosed. These catalyst can be used to produce polyurethane foam having the following desirable characteristics: a) very low chemical emissions over a wide range of environmental conditions and isocyanate indexes (e.g., indexes as low as 65 but higher than 60) while meeting all physical property requirements; b) sufficient hydrolytic stability to maintain the catalyst covalently bound to foam without leaching of tertiary amine catalyst when foam is exposed to water or aqueous solutions even at temperatures higher than ambient (temperature range 25° C. to 90° C.); and c) stable contact interface between the polyurethane polymer and other polymers (for example polycarbonate) with minimal migration of tertiary amine catalyst from polyurethane polymer to other polymers yielding no noticeable polymer deterioration at the point of contact even under conditions of heat and humidity. 114-. (canceled)15. A method for making a polyurethane foam comprising contacting at least one polyol and at least one isocyanate in the presence of at least one catalyst composition and at least one blowing catalyst , wherein the at least one catalyst composition comprises at least one compound with the general formula A-NR1R2 wherein A is [MeN—(CH)]N—(CH)— and R1 and R2 are both CH—CH(OH)—CH , or A is [MeN—(CH)]N—(CH)— and R1 and R2 are both CH—CH—OH.16. The method of wherein the at least one compound comprises at least one member selected from the group consisting of N claim 15 ,N-bis(3-dimethylaminopropyl)-N-[3-aminopropyl-N′ claim 15 ,N′-bis(2-hydroxypropyl)]amine and N claim 15 ,N-bis(3-dimethylaminopropyl)-N-[3-aminopropyl-N′ claim 15 ,N′-bis(2-hydroxyethyl)]amine.17. The method of wherein the at least one blowing catalyst comprises at least one member selected from the group consisting of N claim 15 ,N claim 15 ,N′- ...

MATERIALS EXHIBITING BIOMIMETIC CARBON FIXATION AND SELF-REPAIR

A composition can photocatalytically reduce carbon dioxide. 1. A composition comprising:a polymer matrix including a catalyst configured to generate additional material to the polymer matrix from carbon dioxide with light energy, chemical energy or electrical energy to form formaldehyde or a formaldehyde product.2. The composition of claim 2 , wherein the catalyst includes a chloroplast claim 2 , a nanocatalyst claim 2 , or a colloidal battery.3. The composition of claim 1 , further comprising a chloroplast in a hydrogel.4. The composition of claim 3 , further comprising a nanoparticle.5. The composition of claim 4 , wherein the nanoparticle includes ceria.6. The composition of claim 3 , wherein the composition further comprises a glucosidase claim 3 , a glucose dehydrogenase or a hexokinase.7. The composition of claim 3 , further comprising a graphene oxide.8. The composition of claim 3 , further comprising an acrylamide.9. The composition of claim 1 , wherein the formaldehyde product is urea formaldehyde or polyoxymethylene. This application is a divisional application of U.S. application Ser. No. 16/591,596, filed on Oct. 2, 2019, which claims the benefit of prior U.S. Provisional Patent Application No. 62/740,376, filed Oct. 2, 2018, each of which is incorporated by reference in its entirety.This invention was made with Government support under Grant No. DE-FG02-08ER46488 awarded by the Department of Energy (DOE). The Government has certain rights in the inventionThe invention relates to materials capable of carbon dioxide fixation.Carbon dioxide is the main source for production of many chemicals including methanol and methane. Strategies for COreduction yield various products with different yield and selectivity. However, these approaches share the high energy consumption rates, using valuable reactants such as H, and possibly emitting more net COto atmosphere.In one aspect, a method of sequestering carbon dioxide can include exposing a composition including a ...

Octahydroanthracene Compound, Preparation Method and Application Thereof

An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound. 2. The octahydroanthracene compound and the pharmaceutically acceptable salts of the octahydroanthracene compound of claim 1 , whereinthe Linker is a substituted/unsubstituted phenyl group, pyridine, furan, pyrrole, thiazole or thiophene; wherein a substituent of the substituted phenyl group, pyridine, furan, pyrrole, thiazole or thiophene is a C1-C6 alkyl group or a C1-C6 alkoxy group.3. The octahydroanthracene compound and the pharmaceutically acceptable salts of the octahydroanthracene compound of claim 1 , wherein the nitrogen-free structural fragment is C1-C10 alkyl group.5. The octahydroanthracene compound and the pharmaceutically acceptable salts of the octahydroanthracene compound of claim 1 , wherein X is hydrogen claim 1 , methyl or ethyl.6. An octahydroanthracene compound and pharmaceutically acceptable salts of the octahydroanthracene compound claim 1 , selecting from:4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] methyl benzoate;4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] benzoic acid;N-hydroxy-4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] benzamide;N-(2-aminophenyl)-4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4 5,6,7,8-octahydro-9-anthryl) carbamoyl] benzamide;N[2-(N,N-diethylamino)]ethyl-4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] benzamide;N-(2-amino) ethyl -4[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5 ...

Surfactant-Enabled Transition Metal-Catalyzed Chemistry

In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions. 114.-. (canceled)16. The method of claim 15 , wherein the transition metal mediated bond formation is performed in an aqueous solvent.17. The method of claim 15 , wherein the transition metal catalyst is selected from an organo-palladium or -nickel reagent claim 15 , organo-copper or -gold reagent claim 15 , organo-rhodium or -iridium complex claim 15 , or an organo-ruthenium claim 15 , -iron claim 15 , or -osmium reagent claim 15 , wherein the catalyst is capable of promoting cross-coupling reactions claim 15 , or other reactions characteristic of catalysis by these metals claim 15 , that form a carbon-carbon claim 15 , carbon-heteroatom or carbon-hydrogen bond.18. The method of claim 15 , wherein Yis methyl.19. The method of claim 15 , wherein the solubilizing agent is selected from the group consisting of Poloxamer 188 claim 15 , Polysorbate 80 claim 15 , Polysorbate 20 claim 15 , Vit E-TPGS claim 15 , Solutol HS 15 claim 15 , PEG-40 Hydrogenated castor oil (Cremophor RH40) claim 15 , PEG-35 Castor oil (Cremophor EL) claim 15 , PEG-8-glyceryl capylate/caprate (Labrasol) claim 15 , PEG-32-glyceryl laurate (Gelucire 44/14) claim 15 , PEG-32-glyceryl palmitostearate (Gelucire 50/13); Polysorbate 85 claim 15 , polyglyceryl-6-dioleate (Caprol MPGO) claim 15 , mixtures of high and low HLB emulsifiers; sorbitan monooleate (Span 80) claim 15 , Capmul MCM claim 15 , Maisine 35-1 claim 15 , glyceryl monooleate claim 15 , glyceryl monolinoleate claim 15 , PEG-6-glyceryl oleate (Labrafil M 1944 CS) claim 15 , PEG-6-glyceryl linoleate (Labrafil M 2125 CS) claim 15 , oleic acid claim 15 , linoleic acid claim 15 , propylene glycol monocaprylate (e.g. Capmul PG-8 or Capryol ...

METHOD FOR PRODUCING ALKYLAMINE DERIVATIVE AND ITS PRODUCTION INTERMEDIATE OF ALKYLAMINE DERIVATIVE

A method for producing an alkylamine derivative having a urea bond represented by formula (I), or a salt thereof, comprises the following steps (a) and (b), step (a): 2. The production method according to claim 1 , wherein in formula (II) claim 1 , R1represents a benzyloxycarbonyl group or a t-butoxycarbonyl group.3. The production method according to claim 1 , wherein in formula (III) claim 1 , R3 and R4 each independently represent a hydrogen atom claim 1 , an unsubstituted Calkyl group claim 1 , a halogen atom claim 1 , or a hydroxy group.4. The production method according to claim 1 , wherein the carbonyl group-introducing reagent is a chloroformic ester claim 1 , carbonyldiimidazole claim 1 , phosgene claim 1 , triphosgene claim 1 , or dimethyl carbonate.5. The production method according to claim 1 , wherein in step (a) claim 1 , the carbonyl group-introducing reagent is carbonyldiimidazole claim 1 , the base is absent claim 1 , and the solvent is one or two or more solvents selected from acetone claim 1 , methyl ethyl ketone claim 1 , methyl isobutyl ketone claim 1 , dichloromethane claim 1 , tetrahydrofuran and acetonitrile.6. The production method according to claim 1 , wherein in step (a) claim 1 , the carbonyl group-introducing reagent is a chloroformic ester claim 1 , the base is one or two or more bases selected from triethylamine claim 1 , pyridine claim 1 , and diisopropylethylamine claim 1 , and the solvent is one or two or more solvents selected from acetonitrile claim 1 , propionitrile claim 1 , dichloromethane claim 1 , acetone claim 1 , N claim 1 ,N-dimethylformamide and tetrahydrofuran.7. The production method according to claim 6 , wherein the chloroformic ester is methyl chloroformate claim 6 , ethyl chloroformate claim 6 , phenyl chloroformate claim 6 , 4-chlorophenyl chloroformate or 4-nitrophenyl chloroformate.9. The production method according to claim 1 , wherein R1represents a tert-butoxycarbonyl group claim 1 , and in step (b) claim 1 , ...

Carbonate derivative production method

The objective of the present invention is to provide a method for producing a carbonate derivative in a safe and efficient manner. The method for producing a carbonate derivative according to the present invention is characterized in comprising irradiating light on a composition containing a C1-4 halogenated hydrocarbon having one or more kinds of halogen atoms selected from the group consisting of a chlorine atom, a bromine atom and an iodine atom, a nucleophilic functional group-containing compound and the specific base in the presence of oxygen.

SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome. 1. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a particle size distribution as follows: d(0.1) of about 2 μm , d(0.5) of about 12 μm , and a d(0.9) of about 49 μm.2. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a d(0.5) particle size distribution ranging from 5 to 20 μm.37-. (canceled)8. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having differential scanning calorimetry (DSC) onset at about 228.28° C. and endotherm at about 230.93° C.9. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a purity in excess of 98% (w/w).10. An oral dosage product comprising the solid drug form of .1112-. (canceled)13. A solid pharmaceutical composition in a unit dosage form suitable for oral administration claim 1 , comprising N-(2 claim 1 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)-cyclopentyl)methyl)urea hydrochloride (ATR-101) in combination with one or more pharmaceutically acceptable carriers or excipients claim 1 , wherein ATR-101 is present in the unit dosage form at a level ranging from about 250-750 mg as measured as the free base form of ATR-101.1428-. (canceled)29. A method of administering a solid pharmaceutical composition of claim 13 , comprising orally administering to a ...

Processes for the preparation of (s)-tert-butyl 4,5-diamino-5-oxopentanoate

Provided are processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate, or a salt, solvate, hydrate, enantiomer, mixture of enantiomers, or isotopologue thereof. Also provided are solid forms of various intermediates and products obtained from the processes.

Oligourea Compounds and Method for Producing Same and Use Thereof

The invention relates to a method for producing oligourea compounds by chain building and depolymerization, and to oligourea dispersions, as well as to their use as fungicides, biocides and/or herbicides. 1. Method for the production of oligomeric urea compounds by reaction of starting compounds each with at least two reactive groups , chosen from the hydroxy and/or thiol group , with di- or polyisocyanatesat a first reaction temperature, in order to construct polyurethane and/or polythiourethane compounds (chain construction),and subsequent depolymerization of the resulting polyurethane and/or polythiourethane compounds in the presence of a primary or secondary diamine or polyamine at a second reaction temperature, wherein the second reaction temperature, in regard to the maximum of the respective temperature, is at least 40° C. higher than the first reaction temperature, in order to obtain compositions having oligomeric urea compounds and the starting compounds with at least two reactive groups, chosen from the hydroxy and/or thiol group.2. Method according to claim 1 , wherein compositions are obtained having oligomeric urea compounds with an oligomerization degree of 2 to 16 and independently of this claim 1 , in terms of the oligourea molecules and excluding the monomers claim 1 , more than 50% and especially more than 80% of all oligourea molecules have oligomerization degrees of 2 to 16 claim 1 , especially 2 to 8.3. Method according to or claim 1 , wherein the production of the polyurethane and/or polythiourethane compounds occurs in the absence of water claim 1 , polyurethane catalysts claim 1 , colorants claim 1 , stabilizers and/or inflators.4. Method according to at least one of the preceding claims claim 1 , wherein the polyurethane and/or polythiourethane compounds are constantly present as liquid claim 1 , dispersed in liquid claim 1 , or in dissolved form under the conditions of the reaction.5. Method according to at least one of the preceding claims ...

EPOXIDATION OF GLYCEROL AND DERIVATIVES THEREFROM

A method producing a surfactant from glycerol by converting glycerol, in a first step, to glycidol, polymerizing glycidol to an aliphatic alcohol and finally substituting a hydroxyl group with a substitute anion. 1. A method of producing a surfactant from glycerol which includes the steps of:(a) converting glycerol to glycidol;{'sub': n', '(2n+2), '(b) polymerizing glycidol to produce an aliphatic alcohol with a molecular formula CHOy, wherein n and y are numerical integers with n in the range 3 to 30 and y=n−1; and'}(c) substituting the hydroxyl moiety of the alcohol with a suitable head group.2. The method according to claim 1 , wherein the conversion of glycerol to glycidol includes the steps of dehydrating glycerol to acrolein (propenal) claim 1 , hydrogenating acrolein to allyl alcohol and epoxidizing allyl alcohol claim 1 , with hydrogen peroxide claim 1 , to glycidol.3. The method according to claim 2 , wherein a zeolite based catalyst is used in the dehydration step.4. The method according to claim 2 , wherein a hydrogenating catalyst claim 2 , including a support and at least one transition metal on the support claim 2 , is used in the hydrogenation step.5. The method according to claim 4 , wherein the at least one transition metal is cadmium claim 4 , silver or iron.6. The method according to claim 2 , wherein an epoxidizing catalyst claim 2 , being a titanium molecular sieve or a gold containing catalyst claim 2 , is used in the epoxidizing step.7. The method according to claim 1 , wherein polymerization claim 1 , in step (b) claim 1 , takes place by heating glycidol claim 1 , in an acidic medium claim 1 , for a predetermined period claim 1 , the length of which is dependent upon the number of carbon atoms (n) required in a tail group of the surfactant.8. The method according to claim 7 , wherein the polymerization step is initiated with boron trifluoride.9. The method according to claim 7 , wherein the tail group has a length in a range n=10 to 20.10. ...

MATERIALS EXHIBITING BIOMIMETIC CARBON FIXATION AND SELF-REPAIR

A composition can photocatalytically reduce carbon dioxide. 1. A method of sequestering carbon dioxide comprising:exposing a composition including a catalyst to carbon dioxide; andreducing the carbon dioxide with the catalyst with light energy, chemical energy or electrical energy to form formaldehyde or a formaldehyde product.2. The method of claim 1 , wherein the catalyst includes a chloroplast claim 1 , a nanocatalyst claim 1 , or a colloidal battery.3. The method of claim 1 , wherein the composition includes a chloroplast in a hydrogel.4. The method of claim 3 , wherein the composition further comprises a nanoparticle.5. The method of claim 4 , wherein the nanoparticle includes ceria.6. The method of claim 3 , wherein the composition further comprises a glucosidase claim 3 , a glucose dehydrogenase or a hexokinase.7. The method of claim 3 , wherein the composition further comprises a graphene oxide.8. The method of claim 3 , wherein the composition further comprises an acrylamide.9. The method of claim 1 , wherein the formaldehyde product is urea formaldehyde or polyoxymethylene.10. A method of self-healing a polymer matrix comprising:exposing a polymer matrix including a catalyst to carbon dioxide and an energy source; andgenerating additional material to the polymer matrix from the carbon dioxide.11. The method of claim 10 , wherein the catalyst includes a chloroplast claim 10 , a nanocatalyst claim 10 , or a colloidal battery.12. The method of claim 10 , wherein the polymer matrix includes a chloroplast in a hydrogel.13. The method of claim 12 , wherein the polymer matrix further comprises a nanoparticle.14. The method of claim 13 , wherein the nanoparticle includes ceria.15. The method of claim 12 , wherein the polymer matrix further comprises a glucosidase claim 12 , a glucose dehydrogenase or a hexokinase.16. The method of claim 12 , wherein the polymer matrix further comprises a graphene oxide.17. The method of claim 12 , wherein the polymer matrix ...

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 6. The compound of any of to for use as a medicament.9. A pharmaceutical composition comprising the compound of any of to and a pharmaceutically acceptable carrier.16. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one or two substituents Rand is further optionally substituted with one or more R.17. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one substituent Rand is further optionally substituted with one or more R.18. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one substituent R.19181818. The compound of any of to or to or the compound for use as a medicament according to any of to or to or the pharmaceutical composition of any of to or to , wherein the cycloalkyl group having from 4 to 7 C atoms which forms part of D is a cyclohexyl group.222121. The compound of any of to or to or the compound for use as a medicament according to any of to or to or the pharmaceutical composition of any of to , wherein each Ris independently selected from —NRR , —NHOH , —NRCOR , —NRSOR , —NRCOOR , —NRCONRR , —NRSONRR , —CONRR , oxo , —Calkylene-NRR , —Calkylene-NHOH , —Calkyene-NRCOR , —Calkylene-NRSOR , —Calkylene-NRCOOR , —Calkylene- ...

On-Demand Rapid Synthesis of Lomustine Under Continuous Flow Conditions

Disclosed herein is a continuous manufacturing process for lomustine that has a short residence time and 63 percent yield. Major advantages of this process are that the total production cost for lomustine is lower, the product is higher quality, and the manufacturing operation is safer for production personnel. 1. A method of producing Lomustine with continuous flow condition , wherein said Lomustine is prepared via a linear sequence of two chemical reactions performed separately in two telescoped flow reactors.3. A system for telescoped Lomustine synthesis , comprising sequentially:a first telescoping chamber mixing cyclohexylamine (1) and 1-chloro-2-isocyanatoethane (2) with triethyalamine (TEA) at 50 C for about 1 minute;a Zaiput liquid-liquid extractor to couple with the first telescoping chamber to remove the base TEA from the first reaction chamber; anda second telescoping chamber for nitrosation of the intermediate product 1-(2-chloroethyl)-3-cyclohexylurea (3) at 25 C for about 8 minutes using tBuONO (5) as the nitrosation agent. This invention was made with government support under CA023168 awarded by National Institutes of Health, and W911NF-16-2-0020 awarded by Army Research Laboratory. The government has certain right in the invention.This disclosure provides a novel method of synthesizing lomustine drug in scalable size under continuous flow conditions. Particularly, lomustine is prepared via a linear sequence of two chemical reactions performed separately in two telescoped flow reactors. The process omits isolation and purification of a labile intermediate, providing tremendous advantages of producing active pharmaceutical ingredient at low cost.Lomustine, a widely used anticancer agent, is a highly lipophilic alkylating agent that produces chloroethyl carbonium ions and carbamylating intermediates in vivo. These electrophilic compounds attack the nucleophilic sites on DNA to form alkylated products. Other anticancer agents such as mitomycin C, ...

PROCESS FOR THE PREPARATION OF ISOBUTYLIDENE DIUREA

Disclosed herein is mixed fertilizer according to the process comprising: reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea, wherein the phase transfer catalyst is a quaternary ammonium salt; and mixing the isobutylidene diurea with at least one of another fertilizer, a secondary nutrient, a trace element, a plant protection agent, a filler, and other fertilizer ingredients, to form the mixed fertilizer. Also disclosed is isobutylidene diurea produced by the process comprising: reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea; wherein the phase transfer catalyst is a quaternary ammonium salt. 1. A mixed fertilizer produced according to the process comprising:reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea, wherein the phase transfer catalyst is a quaternary ammonium salt; andmixing the isobutylidene diurea with at least one of another fertilizer, a secondary nutrient, a trace element, a plant protection agent, a filler, and other fertilizer ingredients, to form the mixed fertilizer.2. The mixed fertilizer according to claim 1 , wherein the phase transfer catalyst is benzyltriethylammonium chloride.3. The mixed fertilizer according to claim 1 , wherein the amount of phase transfer catalyst is 0.5 to 5 mol % of the isobutyraldehyde.4. The mixed fertilizer according to claim 1 , wherein the aqueous solution of the urea contains the urea in an amount of 50 to 85 wt %.5. A process for using a mixed fertilizer claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'applying the mixed fertilizer of to horticultural or agricultural soils.'}6. Isobutylidene diurea produced by the process comprisingreacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form ...

NOVEL KCNQ POTASSIUM CHANNEL AGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. 2. The method according to claim 1 , wherein claim 1 ,{'sub': 2', '3', '2', '3, 'Rand Rare each independently selected from a group consisting of H and D, or Rand Rtogether with the carbon atom to which they attached form cyclopropyl;'}{'sub': 4', '5', '1', '4', '1', '4, 'one of Rand Ris C-Calkyl, and the other is H or C-Calkyl.'}4. The method according to claim 3 , wherein claim 3 ,{'sub': '1', 'Ris H or fluorine;'}{'sub': 2', '3', '2', '3, 'Rand Rare each independently selected from a group consisting of H and D, or Rand Rtogether with the carbon atom to which they attached form cyclopropyl;'}{'sub': 4', '5', '1', '4', '1', '4, 'one of Rand Ris C-Calkyl, and the other is H or C-Calkyl.'}8. The method according to claim 1 , wherein one of Rand Ris methyl claim 1 , and the other is H or methyl.9. The method according to claim 1 , wherein the pharmaceutical acceptable salt is a salt formed by reacting the compound with an acid.10. The method according to claim 9 , wherein the acid is selected from a group consisting of maleic acid claim 9 , succinic acid claim 9 , citric acid claim 9 , tartaric acid claim 9 , fumaric acid claim 9 , formic acid claim 9 , acetic acid claim 9 , propanoic acid claim 9 , propandioic acid claim 9 , oxalic acid claim 9 , benzoic acid claim 9 , phthalic acid claim 9 , methanesulfonic acid claim 9 , ...

6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES

The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and Rare as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 2. The compound according to wherein L is —C(O)NH—.3. The compound according to claim 2 , said compound selected from the group consisting of:N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-(trifluoromethyl)isonicotinamide;N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-4-bromo-5-cyclopropyl-1H-pyrazole-3-carboxamide;N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-6-methyl-2-(trifluoromethyl)-pyrimidine-4-carboxamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-6-methyl-2-(trifluoromethyl)-pyrimidine-4-carboxamide;N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(R)—N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(S)—N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(S)—N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-4-chlorobenzamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-chlorobenzamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-methylisonicotinamide;(S)-2-acetamido-N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)isonicotinamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-ethoxyisonicotinamide;(S ...

Method for producing meta-xylylenediisocyanates

A method for producing meta-xylylenediisocyanates includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound represented by general formula (1) below are allowed to react in the presence of an acidic liquid to produce a bisamide compound; a dehalogenation step in which in the bisamide compound, the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom; and a thermal decomposition step in which the bisamide compound from which the halogen atom is eliminated is subjected to thermal decomposition. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 14, the acidic liquid has an inorganic acid concentration of more than 90 mass %, and the reaction temperature is more than 10° C. General formula (1): wherein R 1 represents an alkoxy group or an amino group.

PHOSPHINE LIGANDS FOR CATALYTIC REACTIONS

The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions. 130-. (canceled)33. The method of claim 31 , wherein X is attached to an atom of Aradjacent to the atom bonded to Ar.35. The method of claim 34 , wherein Rand Rare hydrogen.36. The method of claim 34 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 34 , 4- claim 34 , 5- claim 34 , 6- claim 34 , or 7-membered spirocyclic ring containing 0 claim 34 , 1 claim 34 , or 2 ring heteroatoms.38. The method of claim 31 , wherein Arand Arare each aryl.39. The method of claim 31 , wherein Aris substituted with two Rand Aris substituted with three R.40. The method of claim 31 , wherein Ris alkyloxy and wherein Ris alkyl.41. The method of claim 31 , wherein Ris isopropyl.43. The method of claim 42 , wherein Rtogether with Rform a 5-membered spiro ring containing two heteroatoms.44. The method of claim 43 , wherein the two heteroatoms are each oxygen.45. The method of claim 31 , wherein R claim 31 , R claim 31 , R claim 31 , and Rare each methyl.48. The method of claim 47 , wherein the compound is selected from the group consisting of:2,2,6,6-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphinane;2,2,6,6-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphinan-4-one;2,2,6,6-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphinan-4-ol;7,7,9,9-tetramethyl-8-(2′,4′,6′-triisopropylbiphenyl-2-yl)-1,4-dioxa-8-phosphaspiro[4.5]decane;8,8,10,10-tetramethyl-9-(2′,4′,6′-triisopropylbiphenyl-2-yl)-1,5-dioxa-9-phosphaspiro[5.5]undecane;3,3,8,8,10,10-hexamethyl-9-(2′,4′,6′-triisopropylbiphenyl-2-yl)-1,5-dioxa-9-phosphaspiro[5.5]undecane;1-(2′-(dimethylamino)-6′-methoxybiphenyl-2-yl)-2,2,6,6-tetramethylphosphinan-4-one;1-(2′,6′-bis(dimethylamino)biphenyl-2-yl)-2,2,6,6-tetramethylphosphinan-4-one;1-(2′,6′-dimethoxybiphenyl-2 ...

PROCESS FOR THE PREPARATION OF URETHANES

Urethanes are prepared by oxidative carbonylation of at least one amino compound in the presence of carbon monoxide, oxygen and organic, at least one hydroxyl-group-carrying compound. The carbonylation is carried out in the absence of halogen-containing promoters. The carbonylation is also carried out in the presence of a metal complex catalyst which contains neutral bidentate N-chelate ligands of the (N˜N) type, two monoanionic N,O-chelate ligands of the general type (N˜O) or tetradentate dianionic chelate ligands (O˜N˜N˜O). 110-. (canceled)12. The process of claim 11 , wherein the metal complex catalyst is used in a concentration of from 0.1 to 10 mol % claim 11 , based on one mole of amino groups.13. The process of claim 11 , wherein the carbonylation is carried out in methanol claim 11 , ethanol claim 11 , n-butanol claim 11 , or 2 claim 11 ,2 claim 11 ,2-trifluoroethanol.14. The process of claim 11 , wherein ureas groups are formed during the carbonylation claim 11 , wherein these urea groups subsequently react further claim 11 , partially or completely claim 11 , with the organic hydroxyl-group-containing compound by alcoholysis to give the corresponding urethanes.15. The process of claim 11 , in which an aliphatic claim 11 , cycloaliphatic and/or aromatic mono- or di-amino compound is used.16. The process of claim 11 , in which the carbonylation is carried out in the absence of a halogenated solvent.17. A process for the preparation of isocyanates claim 11 , comprising:a) preparing a urethane by carbonylation by the process of 1, andb) thermally cleaving the urethane to obtain the isocyanate.18. The process of claim 17 , wherein the carbonylation and the thermal cleavage take place in one process step. The invention relates to a process for the preparation of urethanes and/or ureas by oxidative carbonylation of amino compounds in the presence of carbon monoxide and oxygen as oxidizing agents and, particularly in the case of the urethanes, in the presence of ...

ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE

The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose. 1. A method of carrying out an organic reaction in a solvent containing at least 90% by weight , in particular at least 97% by weight , based on the total weight of the solvent , of water , which method comprises reacting the reagents in said solvent in the presence of a cellulose derivative which is selected from the group consisting of cellulose modified with one or more alkylene oxides or other hydroxyalkyl precursors , and alkylcellulose;where the organic reaction is not a polymerization or oligomerization reaction of olefinically unsaturated compounds.2. The method as claimed in claim 1 , where the cellulose derivative has a viscosity of from 1 to 150000 mPa·s claim 1 , in particular 2 to 100000 mPa·s claim 1 , specifically 2 to 10000 mPa·s claim 1 , determined as a 2% by weight aqueous solution claim 1 , relative to the weight of water.3. The method as claimed in claim 1 , where in the cellulose derivative 5 to 70% claim 1 , in particular 10 to 60% claim 1 , especially 15 to 50% of the hydrogen atoms in the hydroxyl groups of the cellulose on which the cellulose derivative is based are replaced by a hydroxyalkyl and/or alkyl group.4. The method as claimed in claim 1 , where the cellulose modified with one or more alkylene oxides or other hydroxyalkyl precursors is selected from the group consisting of hydroxyalkylcelluloses which are celluloses in which a part of the hydrogen atoms of the OH groups is replaced by a C-C-hydroxyalkyl group; hydroxyalkylalkylcelluloses which are celluloses in which a part of the hydrogen atoms of the OH groups is replaced by a C-C-hydroxyalkyl group and a part of the hydrogen atoms of the OH groups is replaced by a C-C-alkyl group; and alkylcelluloses which are celluloses in which a part of the hydrogen atoms of the OH groups is replaced by a C-C-alkyl group.5. ...

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

UREAURETHANES FOR RHEOLOGY CONTROL

The present invention relates to ureaurethanes of the following formula (I) 2. The urea urethane as claimed in claim 1 , characterized in that{'sup': '1', 'the Rradical is a monounsaturated alkenyl radical having 16 to 20 carbon atoms,'}{'sup': '2', 'the Rradical is a saturated branched alkyl radical having 10 to 16 carbon atoms or a monounsaturated alkenyl radical having 16 to 20 carbon atoms,'}{'sup': '3', 'the n Rradicals are independently one or more radicals selected from the structural units (IIa-m) and (IIa-p), and'}{'sup': '4', 'the n+1 Rradicals are independently one or more radicals of the structural units (IIIa) and (IIIb).'}3. The urea urethane as claimed in claim 1 , characterized in that{'sup': '1', 'the Rradical is an unbranched octadecenyl radical,'}{'sup': '2', 'sub': 10', '14, 'the Rradical is a branched or unbranched C-C-alkyl radical or an unbranched octadecenyl radical,'}{'sup': '3', 'the n Rradicals are a radical of the structural unit (IIa-m), and'}{'sup': '4', 'the n+1 Rradicals are independently one or more radicals of the structural units (IIIa) and (IIIb).'}4. The urea urethane as claimed in claim 1 , characterized in that{'sup': '4', 'the structural units (IIIa) and (IIIb) are present in the n+1 Rradicals in a molar ratio of 40:60 up to a molar ratio of 100:0.'}5. The urea urethane as claimed in claim 1 , characterized in that{'sup': 1', '2, 'Rand Rare a mono- or polyunsaturated, branched or unbranched alkenyl radical having 16 to carbon atoms.'}6. The urea urethane as claimed in claim 1 , characterized in that Ris oleyl.7. The urea urethane as claimed in claim 1 , characterized in that R═R.8. A urea urethane composition comprising one or more urea urethanes of claim 1 , characterized in that{'sup': 1', '2, 'the proportion by weight of the urea urethanes of the formula (I) in which both Rand Rradicals are unsaturated is 10% to 100%, based on the totality of the urea urethanes of the formula (I), and'}{'sup': '1', 'the proportion by weight ...

PROCESS FOR PREPARATION OF CARMUSTINE

The present invention relates to an improved process for preparation of carmustine (I). The present invention also relates to preparation of 1,3-bis(2-chloroethyl)urea (II) an intermediate used in preparation of carmustine. 3. The process according to claim 1 , wherein step (a) is carried out in presence of a reagent selected from group consisting of 1 claim 1 ,1-carbonyldiimidazole claim 1 , triphosgene and phenyl chloroformate.4. The process according to claim 2 , wherein step (b) is carried out in presence of nirosating reagent.5. The process according to claim 4 , wherein nitrosating reagent is selected from group consisting of di-nitrogen trioxide claim 4 , sodium nitrite and acid.6. The process according to claim 5 , wherein acid is selected from hydrochloric acid claim 5 , sulphuric acid claim 5 , formic acid and acetic acid.7. The process according to claim 4 , wherein nitrosating reagent is sodium nitrite and sulphuric acid.9. The process according to claim 8 , wherein base used in step (a) is triethylamine.10. The process according to claim 8 , wherein solvent used in step (b) is dichloromethane and water.11. The process according to claim 2 , wherein step (a) is carried out in presence of a reagent selected from group consisting of 1 claim 2 ,1-carbonyldiimidazole claim 2 , triphosgene and phenyl chloroformate. This application is related to Indian Provisional Application No. IN 201621013299 filed 16 Apr. 2016 and is incorporated herein in its entirety.The present invention relates to an improved process for preparation of carmustine (I).The present invention also relates to preparation of 1,3-bis(2-chloroethyl)urea (II)an intermediate used in preparation of carmustine.“Carmustine” [154-93-8] is a medication used mainly for chemotherapy and sometimes for immunosuppression before transplant. It is a nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent. As a dialkylating agent, BCNU is able to form interstrand crosslinks in DNA, which ...

PROCESS FOR THE PREPARATION OF ISOBUTYLIDENE DIUREA

The invention relates to a process comprising: reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea. Preferably, the phase transfer catalyst is a quaternary ammonium salt, more preferably benzyltriethylammonium chloride. Even more preferably, the process is performed in one pot. 1. A process for forming isobutylidene diurea , comprising:reacting isobutyraldehyde with an aqueous solution of urea in the presence of a phase transfer catalyst to form isobutylidene diurea.2. The process according to claim 1 , wherein the reacting of the isobutyraldehyde with the aqueous solution of urea in the presence of the phase transfer catalyst is performed in one pot.3. The process according to claim 1 , wherein the phase transfer catalyst is a quaternary ammonium salt.4. The process according to claim 1 , wherein the phase transfer catalyst is benzyltriethylammonium chloride.5. The process according to claim 1 , wherein the amount of phase transfer catalyst is 0.5 to 5 mol % of the isobutyraldehyde.6. The process according to claim 1 , wherein the amount of phase transfer catalyst is 1 to 5 mol % of the isobutyraldehyde.7. The process according to claim 1 , wherein the amount of phase transfer catalyst is 2 to 4 mol % of the isobutyraldehyde.8. The process according to claim 1 , wherein the aqueous solution of the urea contains the urea in an amount of 50 to 85 wt %.9. The process according to claim 1 , further comprising isolating the isobutyilidene diurea to obtain isolated isobutylidene diurea.10. The process according to claim 1 , further comprising mixing the formed isobutylidene diurea or the isolated isobutylidene diurea with another fertilizer and/or with a secondary nutrient and/or with a trace element and/or with a plant protection agent and/or with a filler and/or with other fertilizer ingredients to form a mixed fertilizer.11. A mixed fertilizer obtainable by the process of .12. The use of ...

Method for Enhancing the Rate of the Formation of the Reaction Product of a Carboxylic Acid and Urea via Acid Addition

The present invention is directed to a method for enhancing the rate of formation of the reaction products of a carboxylic acid and a urea having the formula: 2. The method of wherein said carboxylic acid is formic acid.3. The method of wherein said carboxylic acid has the formula RCOOH where R is selected from the group consisting of hydrogen claim 1 , substituted and unsubstituted alkyl claim 1 , allyl claim 1 , vinyl and alkoxyl groups having from 1 to 6 carbon atoms claim 1 , substituted and unsubstituted phenyl groups and the halides.4. The method of wherein said urea has the formula (NHR)CO where each Ris the same or different and is selected from the group consisting of hydrogen claim 1 , substituted and unsubstituted alkyl groups having from 1 to 6 carbon atoms claim 1 , substituted and unsubstituted alkoxyl groups having from 1 to 6 carbon atoms claim 1 , substituted and unsubstituted phenyl groups and the halides.5. The method of claim 1 , wherein said solution includes 0.1-20 wt. % acid.6. The method of claim 1 , wherein said solution includes 0.1-10 wt. % acid.7. The method of claim 1 , wherein a reaction product N claim 1 ,N′-diformylurea is formed by providing a solution including formic acid as said carboxylic acid and urea as said urea.8. A formulation for enhancing plant growth comprising {'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'said reaction product of , wherein said formulation does not contain any pH modifiers.'}, 'at least one solvent and'}9. The formulation of wherein said pH modifiers are hydroxide-containing compounds.10. The formulation of wherein said pH modifier is potassium hydroxide.11. The formulation of wherein said formulation further comprises a vegetable oil and a surfactant.12. The formulation of wherein said vegetable oil is selected from the group consisting of sunflower oil and soybean oil claim 11 , and said surfactant is selected from the group consisting of organic polyphosphates claim 11 , siloxanes claim 11 , and ...

METHOD FOR PRODUCING AMIDES OR POLYAMIDES BY USING AROMATIC CARBAMATES BY WAY OF ISOCYANATES AS PRECURSORS THROUGH CATALYZED THERMAL PROCESSES AND METHOD FOR PRODUCING AROMATIC CARBAMATE PRECURSORS FROM AROMATIC AMINES

The present invention is directed to a process for preparing amides or polyamides by replacing isocyanate starting materials of a catalyzed thermal reaction with aromatic carbamates. Through the catalyzed thermal process involving a non-isocyanate precursor of the present invention, efficiency for producing amides or polyamides can be significantly improved, and the impure side products produced from a side reaction of isocyanate can be greatly curtailed. Hence, amides or polyamides of high purity and yield can be achieved. The invention also relates to a process for preparing aromatic carbamates, the new non-isocyanate precursors for amides or polyamides. 1. A method for preparing an amide or polyamide , comprising the steps of:(a) thermally cracking an aromatic carbamate in a polymerization solvent, to form an aromatic isocyanate solution;(b) subjecting the aromatic isocyanate to a self-condensation reaction in the presence of a carbodiimide (CDI) catalyst, to form an aromatic carbodiimide;(c) reacting the aromatic carbodiimide with a carboxylic acid, to form a reaction intermediate aromatic N-acyl urea; and(d) thermally cracking the aromatic N-acyl urea, to form the aromatic isocyanate and the amide or polyamide product;wherein Steps (b) to (d) are performed repeatedly.2. The method according to claim 1 , wherein in Steps (b) to (d) claim 1 , a sequential self-repetitive reaction (SSRR) is carried out.3. The method according to claim 1 , wherein the carboxylic acid is selected from the group consisting of a monocarboxylic acid claim 1 , a dicarboxylic acid claim 1 , and a mixture thereof.4. The method according to claim 3 , wherein the dicarboxylic acid is selected from the group consisting of an aliphatic diacid claim 3 , an aromatic diacid claim 3 , an aryl aliphatic diacid claim 3 , and a mixture thereof.5. The method according to claim 3 , wherein the carboxylic acid is selected from the group consisting of acetic acid claim 3 , benzoic acid claim 3 , oxalic ...

ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE

The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose. 1. A method of carrying out an organic reaction in a solvent containing at least 90% by weight , in particular at least 97% by weight , based on the total weight of the solvent , of water , which method comprises reacting reagents in said solvent in the presence of a cellulose derivative , where the cellulose derivative is selected from the group consisting of cellulose modified with one or more alkylene oxides or other hydroxyalkyl precursors , and alkylcellulose;where the organic reaction is not a polymerization or oligomerization reaction of olefinically unsaturated compounds.2. The method as claimed in claim 1 , where the cellulose derivative has a viscosity of from 1 to 150000 mPa·s claim 1 , determined as a 2% by weight aqueous solution claim 1 , relative to the weight of water.3. The method as claimed in claim 1 , where in the cellulose derivative has 5 to 70% of the hydrogen atoms in the hydroxyl groups of the cellulose on which the cellulose derivative is based are replaced by a hydroxyalkyl and/or alkyl group.4. The method as claimed in claim 1 , where the cellulose modified with one or more alkylene oxides or other hydroxyalkyl precursors is selected from the group consisting of hydroxyalkylcelluloses claim 1 , which are celluloses in which a part of the hydrogen atoms of the OH groups is replaced by a C-C-hydroxyalkyl group; hydroxyalkylalkylcelluloses claim 1 , which are celluloses in which a part of the hydrogen atoms of the OH groups is replaced by a C-C-hydroxyalkyl group and a part of the hydrogen atoms of the OH groups is replaced by a C-C-alkyl group; and alkylcelluloses claim 1 , which are celluloses in which a part of the hydrogen atoms of the OH groups is replaced by a C-C-alkyl group.5. The method as claimed in any claim 4 , where the cellulose derivative is selected from the ...

METHOD FOR PRODUCING AMINO ACID AMINOALKYL ESTER OR INORGANIC ACID SALT THEREOF

The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. 2. The method according to claim 1 , wherein the reaction is conducted in presence of at least one acid catalyst selected from the group consisting of organic acids and inorganic acids having a normal boiling point of 0° C. or higher.3. The method according to claim 1 , wherein the compound represented by the general formula (I) is at least one amino acid selected from the group consisting of lysine claim 1 , glutamic acid claim 1 , methionine claim 1 , glycine claim 1 , phenylalanine claim 1 , asparagine claim 1 , alanine claim 1 , leucine claim 1 , isoleucine claim 1 , and valine.4. The method according to claim 2 , wherein the inorganic acid used as an acid catalyst is at least one acid selected from the group consisting of sulfuric acid claim 2 , phosphoric acid claim 2 , nitric acid and boric acid.5. The method according to claim 2 , wherein an acid that forms a salt with the compound represented by general formula (I) or the compound represented by general formula (III) and the acid catalyst are the same acid.6. The method according to claim 1 , whereinin the general formula (I):the substituent is at least one group selected from the group consisting of monovalent aliphatic hydrocarbon groups of at least 1 but not more than 10 carbon atoms, monovalent aromatic cyclic groups of at least 6 but not more than 10 carbon atoms, groups represented by the ...

OPTICAL ISOMERS OF (+) AND (-)-BENZHYDRYL UREAS AND (+) AND (-)-1-[(3-CHLOROPHENYL)-PHENYL-METHYL] UREA, A PHARMACEUTICAL COMPOSITION BASED THEREON AND A METHOD FOR PRODUCING SAID OPTICAL ISOMERS

The invention relates to novel substances, and more particularly to optical isomers of (+) and (−)-benzhydryl ureas of formula (I) and (+) and (−)-1-[(3-chlorophenyl)-phenyl-methyl]urea, a pharmaceutical composition based thereon, and a method for producing said optical isomers and for using same on the basis of the different therapeutic activity exhibited. (I) Where R≠R′ and are selected from the group comprising hydrogen, alkyl, halogen, nitro, amino, alkylamino and hydroxy groups and are situated in the ortho-, para- or meta-positions of the benzene rings. When racemic Halodif 1-[(3-chlorophenyl)-phenyl-methyl]urea was separated using the method according to the invention, optical isomers of (+) and (−)-1-[(3-chlorophenyl)-phenyl-methyl]urea (Halodif isomers) with different degrees of therapeutic activity were produced. 3. A pharmaceutical formulation with anticonvulsive action , containing a therapeutically potent quantity of at least one of the compounds corresponding to formulas (I+) and (I−) in and in a mixture with at least one suitable carrier.5. The method as set in claim 4 , wherein the interaction of diastereomers of tartrates of (+)- and (−)-benzhydrol amines with aqueous solutions of cyanates of alkaline metals takes place at room temperature.6. The method as set in claim 4 , wherein L- or D-tartaric acid is selected as the tartaric acid.7. The method as set in claim 4 , wherein methanol or other aliphatic alcohols are selected as the organic solvent.8. The method as set in claim 4 , wherein the (3-chlorophenyl)-phenyl-methane amine is selected as the racemic mixture of benzhydrol amines represented by formula (III).9. The method as set in claim 8 , wherein that (+)- and (−) diastereomers of tartrates of (3-chlorophenyl)-phenyl-methane amine are produced from the racemic mixture of (3-chlorophenyl)-phenyl-methane amine in the presence of tartaric acids in an organic solvent.10. The method as set in claim 9 , wherein the (+)- and (−) diastereomers of ...

Ethylenically Unsaturated Oligomers

Disclosed are functional polyallophanate oligomers comprising ethylenically unsaturated groups and polymer stabilizer groups selected from hindered amine light stabilizers, ultraviolet light absorbers, antioxidants and dihydrocarbylhydroxylamines. The ethylenically unsaturated groups and the polymer stabilizer groups are bound to the polyallophanate oligomers through allophanate and/or carbamate groups. The polyallophanate oligomers are useful in curable coatings, inks and varnishes. The present polyallophanate oligomers are derived from a) organic polyisocyanates, b) compounds containing at least one isocyanate reactive group and at least one ethylenically unsaturated group and c) polymer stabilizers containing at least one isocyanate reactive group. 1. An oligomer containing one or more ethylenically unsaturated groups bound through allophanate groups and/or carbamate groups and containing one or more polymer stabilizer groups selected from the group consisting of hindered amine light stabilizers , ultraviolet light absorbers , antioxidants and dihydrocarbylhydroxylamines bound through allophanate groups and/or carbamate groups.2. An oligomer according to which is derived from a) one or more organic polyisocyanates claim 1 , b) one or more compounds containing at least one isocyanate reactive group and at least one ethylenically unsaturated group and c) one or more compounds containing at least one isocyanate reactive group and at least one polymer stabilizer group.3. An oligomer according to which is derived froma) one or more polyisocyanates selected from the group consisting of 1,4-diisocyanatobutane, 1,5-diisocyanatopentane, 1,6-diisocyanatohexane (HDI), 1,11-diisocyanatoundecane, 1,12-diisocyanatododecane, 2,2,4- and 2,4,4-trimethyl-1,6-diisocyanatohexane, 1-isocyanato-3,3,5-trimethyl-5-isocyanatomethyl cyclohexane (IPDI), 1,3-diisocyanatocyclobutane, 1,3- and 1,4-diisocyanatocyclohexane, 4,4′-bis-Osocyanatocyclohexylymethane (HMDI), 1,2-bis-(isocyanatomethyl ...

SAFE AND EFFICIENT PROCESS FOR THE PREPARATION OF CARMUSTINE

Carmustine may be safely and efficiently produced by reacting 2-chloroethylamine hydrochloride and 1,1′-carbonyldiimidazole to afford 1,3-bis(2-chloroethyl)-1-urea, followed by nitrosation to give the final product. 2. The process according to claim 1 , wherein said organic solvent is THF.3. The process according to claim 1 , wherein said (a) is conducted at a temperature of from 0 to 10° C. and said (b) is conducted at a temperature of from 20 to 60° C.4. The process according to claim 1 , wherein said (a) is conducted at a temperature of from 0 to 5° C. and said (b) is conducted at a temperature of from 40 to 45° C.5. The process according to 1 claim 1 , wherein at least one of said (a) and said (b) is carried out in the presence of a base.6. The process of claim 1 , further comprising:(c) nitrosation of 1,3-bis(2-chloroethyl)-1-urea to obtain 1,3-bis(2-chloroethyl)-1-nitrosourea.7. The process according to claim 5 , wherein said nitrosation comprises:(c1) dissolving a metal nitrite in an aqueous medium, to obtain an aqueous solution;(c2) adding 1,3-bis(2-chloroethyl)-1-urea and a water-immiscible organic solvent to said aqueous solution, to obtain a tri-phase reaction mixture;(c3) adding formic acid to said tri-phase reaction mixture at a temperature of from 0 to 10° C., to obtain 1,3-bis(2-chloroethyl)-1-nitrosourea; andoptionally isolating said 1,3-bis(2-chloroethyl)-1-nitrosourea from the organic phase.8. The process according to claim 6 , wherein:{'sub': '2', 'said metal nitrite is sodium nitrite (NaNO),'}said water-immiscible organic solvent is a chlorinated hydrocarbon solvent, andsaid (c3) is performed at a temperature of from 0 to 5° C.9. The process according to claim 7 , wherein said water-immiscible organic solvent is dichloromethane.10. The process according to claim 6 , further comprising purifying said 1 claim 6 ,3-bis(2-chloroethyl)-1-nitrosourea by filtration of the organic phase through silica gel.11. The process according to claim 1 , wherein ...

Phosphine ligands for catalytic reactions

The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.

SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome. 1. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a particle size distribution as follows: d(0.1) of about 2 μm , d(0.5) of about 12 μm , and a d(0.9) of about 49 μm.2. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a d(0.5) particle size distribution ranging from 5 to 20 μm.3. The solid drug form of wherein the d(0.5) particle size distribution ranges from 6 to 18 μm.4. The solid drug form of wherein the d(0.5) particle size distribution ranges from 8 to 16 μm.5. The solid drug form of wherein the d(0.5) particle size distribution ranges from 10 to 14 μm.6. The solid drug form of any one of - wherein the d(0.1) particle size distribution is greater than 1 μm.7. The solid drug form of any one of - wherein the d(0.9) particle size distribution is less than 60 μm.8. A solid drug form of N-(2 claim 2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having differential scanning calorimetry (DSC) onset at about 228.28° C. and endotherm at about 230.93° C.9. A solid drug form of N-(2 claim 2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a purity in excess of 98% (w/w).10. An oral dosage product comprising the solid drug form of any one of -.11. The oral dosage product of claim 10 , wherein the product is a capsule containing from 25 to 750 mg of the ...

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

The present invention provides a process of producing a trifluoromcthoxylated aryl or trifluoromothoxylated heteroaryl having the structure: 2. The process of claim 1 , wherein the suitable solvent is chloroform claim 1 , dichloromethane claim 1 , nitromethane claim 1 , dimethylformamide claim 1 , diethyl ether claim 1 , tetrahydrofuran claim 1 , dioxane claim 1 , dichloroethane claim 1 , or hexane.3. The process of claim 1 , wherein the trifluoromethoxylating agent is Togni reagent I or Togni reagent II.4. The process of claim 1 , wherein the base is cesium carbonate or sodium hydride.5. The process of claim 1 , wherein A is a phenyl or pyridine.6. The process of claim 1 , wherein A is a furanyl claim 1 , thiophenyl claim 1 , pyrrolyl claim 1 , thiazolyl claim 1 , imidazolyl claim 1 , pyrazolyl claim 1 , isooxazolyl claim 1 , isothiazolyl claim 1 , naphthalenyl claim 1 , anthracenyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridazinyl claim 1 , indolyl claim 1 , indolinyl claim 1 , benzofuranyl claim 1 , benzothiophenyl claim 1 , or quinolonyl.1035.-. (canceled)38. The process of claim 2 , wherein the base is cesium carbonate or sodium hydride.39. The process of claim 3 , wherein the base is cesium carbonate or sodium hydride.40. The process of claim 2 , wherein A is a phenyl or pyridine.41. The process of claim 3 , wherein A is a phenyl or pyridine.42. The process of claim 4 , wherein A is a phenyl or pyridine.43. The process of claim 2 , wherein A is a furanyl claim 2 , thiophenyl claim 2 , pyrrolyl claim 2 , thiazolyl claim 2 , imidazolyl claim 2 , pyrazolyl claim 2 , isooxazolyl claim 2 , isothiazolyl claim 2 , naphthalenyl claim 2 , anthracenyl claim 2 , pyrimidinyl claim 2 , pyrazinyl claim 2 , pyridazinyl claim 2 , indolyl claim 2 , indolinyl claim 2 , benzofuranyl claim 2 , benzothiophenyl claim 2 , or quinolonyl.44. The process of claim 3 , wherein A is furanyl claim 3 , thiophenyl claim 3 , pyrrolyl claim 3 , thiazolyl claim 3 , imidazolyl ...

PHOSPHINE LIGANDS FOR CATALYTIC REACTIONS

The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands. 149-. (canceled)53. The compound of claim 52 , wherein X is attached to an atom of Aradjacent to the atom bonded to Ar.58. The compound according to claim 57 , wherein X comprises a 4-membered ring.59. The compound according to claim 57 , wherein X comprises a 5-membered ring.60. The compound according to claim 57 , wherein X comprises a 7-membered ring or an 8-membered ring.61. The compound according to claim 57 , wherein R claim 57 , R claim 57 , R claim 57 , and Rare selected from the group consisting of alkyl claim 57 , phenyl claim 57 , and heteroaryl claim 57 , or wherein Ror Rtogether with Ror Rform a ring.64. The compound of claim 63 , wherein the compound is selected from the group consisting of:1-(biphenyl-2-yl)-2,2,7,7-tetramethylphosphepan-4-one;1-(biphenyl-2-yl)-2,2,7,7-tetramethylphosphepane;2,2,7,7-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphepan-4-one;2,2,7,7-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphepane;2,2,8,8-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphocan-4-one; and2,2,8,8-tetramethyl-1-(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphocane.67. The compound of claim 66 , wherein the compound is selected from the group consisting of:{'sup': '3,7', '1,3,5,7-tetramethyl-8-(2′,4′,6′-triisopropylbiphenyl-2-yl)-2,4,6-trioxa-8-phosphatricyclo[3.3.1.1]decane; and'}{'sup': '3,7', '8-(biphenyl-2-yl)-1,3,5,7-tetramethyl-2,4,6-trioxa-8-phosphatricyclo[3.3.1.1]decane.'}68. 1-(2-(2 claim 66 ,2 claim 66 ,6 claim 66 ,6-tetramethylphosphinan-1 -yl)phenyl)-1H-pyrrole.71. The compound according claim 69 , wherein ring A is a 4- claim 69 , 5- claim 69 , 6- claim 69 , 7- claim 69 , or 8-membered ring claim 69 , and wherein each of the ring atoms in addition to the phosphorus and 2 carbon ring atoms of formula (Ia) are carbon.72. The compound according to ...

METHOD FOR THE STEREOISOMERIZATION OF CHIRAL COMPOUNDS

The present invention provides a novel method for the controlled stereoisomerization (comprising the stereo-conversion of chiral compounds to racemates, non-racemic mixtures and mixtures of epimers). The method of the invention provides the fully controlled generation of mixtures of different ratios of (S) and (R) stereoisomers, both enantiomers and diastereomers, of a given compound or a mixture of compounds. Such mixtures and isotopically labeled variants of said mixtures provided by the present invention are useful as an authenticity or external or internal standards in various biochemical and medical applications. Further, with the method of the invention it is possible to generate specific stereoisomers from some amino acids as well as degradation and oxidation products thereof which were previously not available. Thence, the invention provides in additional aspects the generation of a group of previously unavailable stereoisomers (enantiomers, epimers, and mixtures thereof such as a racemate) with amino acid type structures. 1. A method for the stereoisomerization (racemization or epimerization) of a chiral compound , the method comprising the steps: (aa) the chiral compound which contains at least one stereogenic carbon atom;', '(bb) a stereoisomerization tag; and', '(cc) optionally a buffer; and, 'a) providing a mixture comprising(b.1) heating the mixture to a temperature from 50 to 200° C. for 30 minutes to 24 hours;or(b.2) treating the mixture in a microwave at 200 to 400 W for 1 min to 6 h, at a temperature from 50 to 300° C.2. The method according to claim 1 , wherein the heating in step (b.1) is at a temperature range from 55 to 95° C.6. The method according to claim 5 , wherein the stereoisomerization-tag is selected from aminophenyl-N-hydroxysuccinimidyl carbamate (AC) claim 5 , 3-aminopyridyl-N-hydroxysuccinimidyl carbamate (APC) and claim 5 , preferably claim 5 , 6-aminoquinolinyl-N-hydroxysuccinimidyl carbamate (AQC claim 5 , AccQ).7. The method ...

SEPARATING AGENT AND MANUFACTURING METHOD THEREOF

An embodiment of the present invention is a separating agent wherein a group represented by a chemical formula of: 3. A separating agent manufactured by the manufacturing method of a separating agent as claimed in .4. A column comprising the separating agent as claimed in .5. A liquid chromatograph comprising the column as claimed in .6. A separation method comprising a step of separating an enantiomer or a diastereomer by using the column as claimed in . An embodiment of the present invention relates to a separating agent, a manufacturing method of a separating agent, a column, a liquid chromatograph, a separation method, and a compound.In recent years, the presence of various enantiomers has been confirmed within the bodies of higher order animals such as mammals, and the important functions that each enantiomer serves are being elucidated. Among amino acids, large amounts of L-amino acids are present inside a body as constituents of proteins or nutrient sources whereas trace amounts of D-amino acids that are enantiomers thereof are frequently present inside the body. Because of this, when D-amino acids are analyzed, interference from a wide variety of peptides or amino compounds frequently occurs. Furthermore, mass spectrometry used for analysis at a high resolution is such that separation of enantiomers is impossible in principle, and hence, development of an optical resolution technique at a high resolution is desired to conduct accurate quantitative analysis.Non-Patent Document 1 discloses a method for optically resolving fluorescently derivatized amino acids by using SUMICHIRAL (registered trademark) OA2500S (produced by Sumika Chemical Analysis Service, Ltd.).Patent Document 1 discloses a two-dimensional HPLC wherein a column for optical resolution is combined with a reversed-phase column.However, in addition to the elution order of D-bodies and L-bodies of amino acids not being identical, there is a problem of a low resolution between peaks originating from ...

Method For Preparing Biuret Polyisocyanate

A method for continuously preparing biuret polyisocyanate, comprising: a mixed solution of a diisocyanate and a catalyst with water vapour, in an aerosol form, are continuously reacted in a first reactor; the product obtained therefrom is brought into a second reactor for a further reaction; a tail gas from the second reactor is condensed and refluxed, and the non-condensable gas is brought into a tail gas treatment system; a reaction liquid obtained in the second reactor is further reacted in a third reactor; and then separation is performed for removing monomers, so as to obtain biuret polyisocyanate. 1. A method for continuously preparing biuret polyisocyanate , comprising the following steps:a) a mixed solution of a diisocyanate and a catalyst, and water vapour, in an aerosol form, are continuously reacted in a first reactor; wherein the continuous phase of the aerosol is the water vapour, the dispersed phase is the mixed solution of the diisocyanate and the catalyst;b) the product obtained in step a) is brought into a second reactor for a further reaction; a tail gas from the second reactor is condensed and refluxed, and the non-condensable gas is brought into a tail gas treatment system;c) the reaction liquid obtained in step b) is further reacted in a third reactor;d) a separation of the reaction liquid obtained in step c) is performed for removing monomers, so as to obtain biuret polyisocyanate.2. The method according to claim 1 , characterized in that: the conversion rate of water vapour in the first reactor is 80-95% claim 1 , based on the water vapour enter into the first reactor.3. The method according to claim 2 , characterized in that: the total conversion rate of water vapour after step b) is higher than 95% claim 2 , based on the water vapour enter into the first reactor.4. The method according to claim 2 , characterized in that: the residence time of the aerosol in the first reactor in step a) is 10-60 min.5. The method according to claim 1 , ...

SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome. 1. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a particle size distribution as follows: d(0.1) of about 2 μm , d(0.5) of about 12 μm , and a d(0.9) of about 49 μm.2. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a d(0.5) particle size distribution ranging from 5 to 20 μm.37-. (canceled)8. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having differential scanning calorimetry (DSC) onset at about 228.28° C. and endotherm at about 230.93° C.9. A solid drug form of N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride having a purity in excess of 98% (w/w).1012-. (canceled)13. A solid pharmaceutical composition in a unit dosage form suitable for oral administration , comprising N-(2 ,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)-cyclopentyl)methyl)urea hydrochloride (ATR-101) in combination with one or more pharmaceutically acceptable carriers or excipients , wherein ATR-101 is present in the unit dosage form at a level ranging from about 250-750 mg as measured as the free base form of ATR-101.1443-. (canceled)44. A method for treating adrenocortical carcinoma in a patient in need thereof comprising administering to the patient a therapeutically effective amount of the solid drug form of any one of , , or , or the ...

METHOD FOR EXTRACTING CITRULLINE FROM WATERMELON

The present invention relates to the technical field of natural substance extraction. Disclosed is a method for extracting Citrulline from a watermelon. The method for extracting Citrulline from a watermelon in the present invention comprises Raw material pretreatment, ultrasound-enzymatic hydrolysis assisted solvent leaching, and purification steps. The purification step comprises microbial fermentation, ion-exchange resin purification, macroporous adsorption resin discoloration, and crystallization and recrystallization. The method for extracting Citrulline in the present invention is simple, requires a mild condition, and has a good extraction effect on Citrulline. The purity of Citrulline after purification is more than 90%. In addition, the Citrulline extracted by the method in the present invention meets the related health requirements and product quality standards, can be applied to food and health food industries as a raw material, and has natural security advantages.

PROCESSES FOR THE PREPARATION OF (S)-TERT-BUTYL 4,5-DIAMINO-5-OXOPENTANOATE

Provided are processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate, or a salt, solvate, hydrate, enantiomer, mixture of enantiomers, or isotopologue thereof. Also provided are solid forms of various intermediates and products obtained from the processes. 6. The process of claim 5 , wherein the formaldehyde source is paraformaldehyde or 1 claim 5 ,3 claim 5 ,5-trioxane.7. The process of or claim 5 , wherein step (x) occurs in the presence of an acid.8. The process of claim 7 , wherein the acid is p-TsOH claim 7 , MsOH claim 7 , benzenesulfonic acid claim 7 , trifluoromethanesulfonic acid claim 7 , trifluoroacetic acid claim 7 , sulfuric acid claim 7 , or trichloroacetic acid.9. The process of any one of - claim 7 , wherein Ris hydrogen.10. The process of claim 9 , wherein the NH—R(i.e. claim 9 , NH) in step (a) is provided in the form of an ammonia solution in water or MeOH or in the form of gaseous ammonia.11. The process of any one of - claim 9 , wherein Ris a suitable amino protecting group.12. The process of claim 11 , wherein the deprotection of the —NH—Rgroup and the deprotection of the —NH—Rgroup in step (c) are conducted separately.13. The process of claim 11 , wherein the deprotection of the —NH—Rgroup and the deprotection of the —NH—Rgroup in step (c) are conducted simultaneously.14. The process of any one of - claim 11 , wherein Ris benzyl claim 11 , 4-methoxybenzyl claim 11 , or 3 claim 11 ,4-dimethoxybenzyl.15. The process of any one of - claim 11 , wherein Ris (S)-1-phenylethyl.16. The process of any one of - claim 11 , wherein Ris benzyl claim 11 , 4-methoxybenzyl claim 11 , 3 claim 11 ,4-dimethoxybenzyl claim 11 , benzyloxycarbonyl claim 11 , or p-methoxybenzyloxycarbonyl.17. The process of claim 16 , wherein Ris benzyloxycarbonyl.18. The process of any one of - claim 16 , wherein step (b) occurs in the presence of t-butyl 2 claim 16 ,2 claim 16 ,2-trichloroacetimidate.19. The process of any one of - claim 16 , wherein step (b) ...

BENZAMIDE DERIVATIVE

The present invention relates to a benzamide derivative of general formula I, a drug composition containing same and a use thereof as a drug, wherein the definitions of R, Z and Q are as described in the description. 15. A pharmaceutical composition claim 1 , comprising the compound of formula I claim 1 , or the tautomer claim 1 , the optical isomer and the pharmaceutically acceptable salt thereof according to .16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. A pharmaceutical composition claim 14 , comprising the compound claim 14 , or the tautomer claim 14 , the optical isomer and the pharmaceutically acceptable salt thereof according to .21. A method for preventing and/or the treating symptoms or diseases mediated by p38 kinase activity or mediated by the cytokines produced by p38 kinase activity comprising administering to a subject a therapeutically effective amount of the compound of formula I claim 1 , or the tautomer claim 1 , the optical isomer and the pharmaceutically acceptable salt thereof according to .22. A method for preventing and/or the treating symptoms or diseases mediated by p38 kinase activity or mediated by the cytokines produced by p38 kinase activity comprising administering to a subject a therapeutically effective amount of the compound claim 14 , or the tautomer claim 14 , the optical isomer and the pharmaceutically acceptable salt thereof according to .23. The method according to claim 21 , wherein the disease is selected from inflammatory disease.24. The method according to claim 22 , wherein the disease is selected from inflammatory disease.25. The method according to claim 21 , wherein the disease is selected from rheumatoid arthritis claim 21 , chronic lung obstruction claim 21 , cardiovascular disease claim 21 , gout claim 21 , psoriasis claim 21 , asthma claim 21 , tumor claim 21 , diabetes mellitus claim 21 , arteriosclerosis and Crohn's disease.26. The method according to claim 22 , wherein the disease is selected from ...

Substituted Ureas and Methods of Making and Using Same

The invention relates to substituted ureas, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof. 23-. (canceled)6. (canceled)10. The compound of claim 1 , wherein A is selected from the group consisting of 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 5-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 6-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 7-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 8-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 5-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 6-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 7-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 8-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-1-yl claim 1 , 5-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 6-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 7-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 8-fluoro-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 5-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 6-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , 7-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen-2-yl claim 1 , and 8-hydroxy-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalen 2 yl.11. The compound of claim 1 , wherein Bis H claim 1 , and wherein Bis selected from the group consisting of 3-thienyl claim 1 , 2-thienyl claim 1 , 2-chloro-4-fluorophenyl claim 1 , 4-chloro-2-fluorophenyl claim 1 , 4-methoxyphenyl claim 1 , 4-hydroxyphenyl claim 1 , and phenyl. ...

Compositions Comprising TPGS-750-M

In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions. 114.-. (canceled)16. The compound of wherein n is an integer selected from 10 to 50.17. The compound of wherein n is an integer selected from 16 to 20.18. The compound of claim 15 , wherein n is 15.20. The mixture of claim 19 , where n is 15.21. The mixture of claim 19 , wherein the transition metal catalyst is selected from an organo-palladium or -nickel reagent claim 19 , organo-copper or -gold reagent claim 19 , organo-rhodium or -iridium complex claim 19 , or an organo-ruthenium claim 19 , -iron claim 19 , or -osmium reagent claim 19 , wherein the catalyst is capable of promoting cross-coupling reactions claim 19 , or other reactions characteristic of catalysis by these metals claim 19 , that form a carbon-carbon claim 19 , carbon-heteroatom or carbon-hydrogen bond.22. The mixture of claim 19 , wherein the transition metal catalyst comprises less than 5 mole % claim 19 , less than 3 mole % or less than 2 mole % of the mixture.23. The mixture of claim 19 , further comprising (i) a coupling substrate and (ii) a coupling partner.24. The mixture of claim 23 , wherein water is the sole solvent.25. The mixture of claim 24 , wherein the coupling substrate is selected from substituted or unsubstituted alkyl claim 24 , substituted or unsubstituted heteroalkyl claim 24 , substituted or unsubstituted cycloalkyl claim 24 , substituted or unsubstituted heterocycloalkyl claim 24 , substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; and wherein the coupling partner is selected from H claim 24 , substituted or unsubstituted amine claim 24 , substituted or unsubstituted silane claim 24 , substituted or unsubstituted alkyl claim 24 , substituted or ...

Surfactant-Enabled Transition Metal-Catalyzed Chemistry

In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions. 114.-. (canceled)16. The mixture of claim 15 , wherein the non-aqueous solvent or solvent mixtures is selected from the group consisting of methanol claim 15 , ethanol claim 15 , propanol claim 15 , isopropanol claim 15 , n-butanol claim 15 , acetone claim 15 , ethyl acetate claim 15 , methyl acetate claim 15 , THF claim 15 , acetonitrile claim 15 , ethyleneglycol or PEGs claim 15 , dioxane claim 15 , MIBK claim 15 , MEK claim 15 , DMA or mixtures thereof.17. The mixture of claim 16 , wherein the non-aqueous solvent or solvent mixtures is selected from the group consisting of propanol claim 16 , isopropanol claim 16 , acetone claim 16 , THF claim 16 , ethyleneglycol or PEGs or mixtures thereof.18. The mixture of claim 15 , wherein the transition metal catalyst is selected from an organo-palladium or -nickel reagent claim 15 , organo-copper or -gold reagent claim 15 , organo-rhodium or -iridium complex claim 15 , or an organo-ruthenium claim 15 , -iron claim 15 , or -osmium reagent claim 15 , wherein the catalyst is capable of promoting cross-coupling reactions claim 15 , or other reactions characteristic of catalysis by these metals claim 15 , that form a carbon-carbon claim 15 , carbon-heteroatom or carbon-hydrogen bond.19. The mixture of claim 15 , wherein the transition metal catalyst comprises less than 5 mole % claim 15 , less than 3 mole % or less than 2 mole % of the mixture.20. The mixture of claim 15 , further comprising (i) a coupling substrate and (ii) a coupling partner.21. The mixture of claim 16 , wherein the coupling substrate is selected from substituted or unsubstituted alkyl claim 16 , substituted or unsubstituted heteroalkyl claim 16 , ...

REACTIVE AMINE CATALYSTS FOR POLYURETHANE APPLICATIONS

Tertiary amine catalysts having isocyanate reactive groups that are capable of forming thermally stable covalent bonds able to withstand temperatures up to 120° C. are disclosed. These catalyst can be used to produce polyurethane foam having the following desirable characteristics: a) very low chemical emissions over a wide range of environmental conditions and isocyanate indexes (e.g. indexes as low as 65 but higher than 60) while meeting all physical property requirements; b) sufficient hydrolytic stability to maintain the catalyst covalently bound to foam without leaching of tertiary amine catalyst when foam is exposed to water or aqueous solutions even at temperatures higher than ambient (temperature range 25° C. to 90° C.); and c) stable contact interface between the polyurethane polymer and other polymers (for example polycarbonate) with minimal migration of tertiary amine catalyst from polyurethane polymer to other polymers yielding no noticeable polymer deterioration at the point of contact even under conditions of heat and humidity. 1) A catalyst composition comprising at least one compound with the general formula A-NR1R2 wherein A=[Me2N—(CH2)3] 2N—(CH2)3- and R1=R2=—CH2-CH(R3)OH or R=H and R=—CH—CH(R)OH with R3=H. C1-C6 or A=[Me2N—(CH2) 3] 2N—(CH2)3- and R1=H and R2=—CO—NH-A or R1=H and R2=—CO—NH2.2) The composition of wherein the compound comprises at least one member selected from the group consisting of N.N′-bis[bis-N″.N″-(3-dimethylaminopropyl)-N″-(3-aminopropyl)]urea; N.N-bis(3-dimethylaminopropyl)-N-(3-aminopropyl)] urea; N.N-bis(3-dimethylaminopropyl)-N-[3-aminopropyl-N′.N′-bis(2-hydroxypropyl)]amine; N.N-bis(3-dimethylaminopropyl)-N-[3-aminopropyl-N′N′-bis[2-hydroxyethyl)amine; N.N-bis(3-dimethylaminopropyl)-N-[3-aminopropyl-N′-(2-hydroxyethyl)]amine; N.N-bis(3-dimethylaminopropyl)-N-[3-aminopropyl-N′(2-hydroxyethylk)]amine.3) The composition of further comprising at least one blowing catalyst.4) The composition of wherein the blowing catalyst ...

CROSSLINKING COMPONENT FOR BINDER RESINS

This invention relates to a crosslinking component for binder resins which is especially suitable to be used together with epoxy-group containing binders and/or (poly)isocyanates such as blocked (poly)isocyanates and which comprises at least two blocked isocyanate groups per molecule of the crosslinking component whereby at least one of the at least two blocked isocyanate groups is a group according to structural unit (I), wherein the ratio of structural units of formula (II), if present, to structural units of formula (I) is 0.40 or below. The cross-linking component may also be self-cross-linkable. The present invention further relates to a coating composition, e.g. a one-component coating composition comprising the crosslinking component and a method of its manufacture. 3. The crosslinking component according to wherein the crosslinking component is substantially free of structural units (II).4. The crosslinking component according to any one of the preceding to wherein Ris a Cto Calkyl group.5. The crosslinking component according to any one of the preceding to wherein Ris a tert-butyl group.6. The crosslinking component according to any one of the preceding to wherein the number average molecular weight of the crosslinking component is within the range of 350 g/mol to 5000 g/mol.7. A process for producing the crosslinking component according to any one of the preceding to comprising reacting a compound comprising at least two isocyanate groups with an alcohol of the formula R—OH with Rbeing a Cto Chydrocarbyl group whereby the molar amount of the alcohol R—OH is equal to or more than the total molar amount of the compound comprising at least two isocyanate groups.8. A coating composition comprising the crosslinking component according to any one of the preceding to .9. The coating composition of further comprising a binder resin.10. The coating composition of wherein the binder resin is a binder resin comprising epoxy and/or blocked isocyanate groups.11. The ...

NOVEL GEMINI SURFACTANT AND THEIR USE

Disclosed herein are gemini surfactants, and methods for making and using these gemini surfactants. These gemini surfactants may be incorporated in paints and coatings to provide hydrophilic and/or self-cleaning properties. 2. The compound of claim 1 , wherein Ais —H claim 1 , —N[CH—N(Z—CH).X] claim 1 , —NH.X claim 1 , —N[Z—CH] claim 1 , —NH—CH—CH—OH claim 1 , —N(CH—CH—OH).X claim 1 , or —O—Z—CH.3. The compound of claim 1 , wherein Ais —H claim 1 , —N[CH—N(Z—CH).X] claim 1 , —NH.X claim 1 , —N[Z—CH] claim 1 , —NH—CH—CH—OH claim 1 , —N(CH—CH—OH).X claim 1 , or —O—Z—CH.4. The compound of claim 1 , wherein Ais —N[CH—N(Z—CH).X] claim 1 , —NH.X claim 1 , —N[Z—CH] claim 1 , —NH—CH—CH—OH claim 1 , —N(CH—CH—OH).X claim 1 , or —O—Z—CH.5. The compound of claim 1 , wherein Ais —N[CH—N(Z—CH).X] claim 1 , —NH.X claim 1 , —N[Z—CH] claim 1 , —NH—CH—CH—OH claim 1 , —N(CH—CH—OH).X claim 1 , or —O—Z—CH.6. The compound of claim 1 , wherein:{'sup': '1', 'sub': 3', '2', '3, 'Ais —N[Z—CH]or —O—Z—CH;'}{'sup': '2', 'sub': 3', '2', '3, 'Ais —N[Z—CH]or —O—Z—CH;'}{'sup': 3', '+', '−', '+', '−, 'sub': 2', '3', '3', '2', '3', '3, 'Ais —N[CH—N(CH).Br]or —N(Z—CH).Br;'}{'sup': 4', '+', '−', '+', '−, 'sub': 2', '3', '3', '2', '3', '3, 'Ais —N[CH—N(CH).Br]or —N(Z—CH).Br; and'}{'sub': 2', '2', 'k', '2, 'Q is —C(═O)— or —CH—(CH)—CH—.'}7. The compound of claim 1 , wherein Ais —N[Z—CH] claim 1 , Ais —N[Z—CH] claim 1 , Ais —N[CH—N(CH).Br] claim 1 , Ais —N[CH—N(CH).Br] claim 1 , and Q is —C(═)—.8. The compound of claim 1 , wherein Ais —O—C(═O)—COO.Na claim 1 , Ais —O—Z—CH claim 1 , Ais —O—C(═O)—COO.Na claim 1 , Ais —O—Z—CH claim 1 , and Q is —C(═O)—.9. The compound of claim 1 , wherein Ais —N(—CH)—Z—CH.OH claim 1 , Ais —N(—CH)—Z—CH.OH claim 1 , Ais —N(—CH)—Z—CH.OH claim 1 , Ais —N(—CH)—Z—CH.OH claim 1 , and Q is —C(═O)—.10. The compound of claim 1 , wherein Ais —N(Z—CH).Br claim 1 , Ais —O—Z—CH claim 1 , Ais —N(Z—CH).Br claim 1 , Ais —O—Z—CH claim 1 , and Q is —C(═O)—.1221.-. (canceled)23. -33. (Cancelled ...

Polymer with upper critical solution temperature

Aspects generally relate to a temperature responsive polymer, more specifically to a polymer exhibiting an upper critical solution temperature (UCST) in an aqueous solution. In one aspect, a monomer compound includes one or more amide or thioamide groups; one or more ureido or thioureido groups; and one or more ethylenically unsaturated groups. In one aspect, a polymer, such as a homopolymer or a copolymer, is produced by polymerization of the monomer compound. The copolymer is produced by polymerization of the monomer compound and a comonomer, such as a hydrophobic comonomer, a hydrophilic comonomer, a pH responsive comonomer, a light responsive comonomer, and combinations thereof. The polymer exhibits a UCST from about 1° C. to about 100° C. in an aqueous solution at 1 atm. 1. A compound , comprising:one or more amide or thioamide groups;one or more ureido or thioureido groups; andone or more ethylenically unsaturated groups.3. The compound of claim 2 , wherein Q claim 2 , Q claim 2 , Q claim 2 , and Qare each oxygen and wherein R claim 2 , R claim 2 , R claim 2 , and Rare each hydrogen.4. The compound of claim 3 , wherein:{'sup': '1', 'sub': 2', '4, 'Ris —CH—; and'}{'sup': '2', 'sub': '2', 'Ris —CH—.'}5. A method of making the compound of claim 1 , comprising purifying the compound without chromatography.6. A polymer claim 1 , comprising:a plurality of repeating units (n) of monomer units, each monomer unit independently comprising one or more amide or thioamide groups and one or more ureido or thioureido groups, wherein n is an integer from 10 to 200;an optional plurality of repeating units (m) of comonomer units, wherein m is an integer from 0 to 100 and wherein n>m; andat least part of a reversible addition fragmentation chain transfer (RAFT) agent;wherein the polymer is configured to exhibit an upper critical solution temperature from about 1° C. to about 100° C. when present in an aqueous solution at 1 atm.8. The polymer of claim 7 , wherein Q claim 7 , Q ...

METHOD FOR SIMULTANEOUSLY EXTRACTING LYCOPENE AND CITRULLINE FROM WATERMELON

A method for simultaneously extracting Lycopene and Citrulline from a watermelon includes: separating the rind and the pulp of the watermelon, preprocessing the rind, and using the preprocessed rind to extract the Citrulline; subjecting the pulp to biological enzymolysis and filtering, centrifuging a filtrate, using a precipitate and a filter residue obtained after the centrifuging to extract the Lycopene, and using a supernatant obtained after the centrifuging to extract the Citrulline. By using the method for synchronously extracting Lycopene and Citrulline from the watermelon of the present invention, about 0.5 kg of Lycopene (6% content) and more than 1.2 kg of Citrulline which are worthy of nearly ten thousand yuan can be extracted from each ton of imperfect watermelons, the economic benefit of each ton of watermelons can be increased by more than 5000 yuan after extraction costs are deducted, and the method is high in economic benefits. 1. A method for synchronously extracting Lycopene and Citrulline from watermelon , which is characterized in that: separate the rind and pulp of watermelon; the Citrulline is extracted from the rind after pretreatment; process the pulp with biological enzymolysis , then filter to obtain filter residue and filtrate; the filtrate is centrifuged to obtain precipitate and supernatant , the precipitate is mixed with the filter residue above to use to extract Lycopene , and the supernatant is used to extract Citrulline.2. The method for synchronously extracting Lycopene and Citrulline from watermelon according to claim 1 , wherein the process of biological enzymolysis the amount of biological enzyme added is 0.1-0.3% (m/m) claim 1 , with the temperature maintaining at 40-50° C. claim 1 , and then performing 1-2 hours of enzymolysis.3. The method for synchronously extracting Lycopene and Citrulline from watermelon according to claim 2 , wherein the biological enzyme is at least one of pectinase claim 2 , cellulase and protease.4. The ...

Preparation Method of Supercritical Carbon Dioxide Thickener for Tight Oil and Gas Reservoir

The present invention disclosed a method for prparing a thickener for tight oil and gas reservoir, which relieves damages. The technical solution includes the following steps: putting a three-flask in ice; adding perfluoroalkyl alcohol, P-toluenesulfonyl chloride and pyridine; reacting for 3 h at 0-20° C.; adding filter paper; ultrasonic dispersing for 1 h; removing the filter paper; washing the solution for 3-5 times by adding dilute hydrochloric acid to collect the intermediate product (I); adding 1,3-dihydroxy-propane-2-tert-butyl carbamate and the intermediate product (I) in another three-flask; adding potassium carbonate and N,N-dimethylformamide; reacting for 4h at 40° C. to collect the intermediate product (II); adding trifluoroacetic acid and methylene chloride into the intermediate product (II); reacting at 45° C. for 2 h; extracting and vacuum drying; and adding 1,6-hexamethylene diisocyanate; reacting for 2 h to collect the final product (III). 1. A method for preparing a supercritical carbon dioxide thickener for a tight oil and gas reservoir , comprising following steps:(1) preparing P-toluene perfluoroalkyl ethylenesulfonates (TFES), which further comprises following sub-steps: after adding a perfluoroalkyl alcohol and a P-toluenesulfonyl chloride in a three-neck flask, wherein a molar ratio of the perfluoroalkyl alcohol and the P-toluenesulfonyl chloride is 1:1.1-1.2, and adding a pyridine; forming a system; wherein the system has reacted for 3 h under stirring thoroughly; maintaining a temperature at 0-20° C.; adding filter paper and carrying out ultrasonic dispersion for 1 h after a reaction is over; after removing unreacted residue P-toluenesulfonyl chloride and the filter paper; forming a system; washing the system with 15% dilute hydrochloric acid many times to remove the pyridine and collect a white solid; washing the white solid with distilled water for multiple times, drying the white solid by a vacuum drying oven at 40° C. for 3 h to prepare ...

Preparation of isocyanate-substituted allophanates and their use for the preparation of lacquers

Verfahren zur Herstellung von Isocyanatgruppen aufweisenden Allophanaten durch Umsetzung von Urethangruppen aufweisenden organischen Verbindungen mit organischen Polyisocyanaten mit aliphatisch und/oder cycloaliphatisch gebundenen Isocyanatgruppen, in Gegenwart von starken, mit aliphatischen bzw. cycloaliphatischen Isocyanaten ein gemischtes Carbamidsäureanhydrid bildenden Säuren durchführt. Die Allophanatpolyisocyanate können zur Herstellung Polyurethan-Schaumstoffen, Elastomere, Duromeren, Beschichtungen, Verklebungen und Lackierungen eingesetzt werden. Process for the preparation of allophanates containing isocyanate groups by reacting organic compounds containing urethane groups with organic polyisocyanates with aliphatically and / or cycloaliphatically bonded isocyanate groups, in the presence of strong acids which form a mixed carbamic acid anhydride with aliphatic or cycloaliphatic isocyanates. The allophanate polyisocyanates can be used for the production of polyurethane foams, elastomers, thermosets, coatings, bonds and paints.

Process for the preparation of light stable polyisocyanates containing allophanate groups

Procédé de preparation d'allophanates possédant une faible viscosité et des groupes durcissables sous rayonnement actinique

Preparation of radiation hardening allophanate (I) comprises reacting isocyanate group containing compounds (II), hydroxyl functional compounds (III) and optionally further compounds (IV) with NCO reactive groups in presence of a allophanating catalyst, where the proportion of NCO groups of (II) to the OH groups of (III) and optionally (IV) is 1.45:1 to 1.1:1. Preparation of radiation hardening allophanate (I) (having 0.5 wt.% of monomer residue and less than 1 wt.% of isocyanate (NCO) content) comprises reacting NCO group containing compounds (II), hydroxyl functional compounds (III) (which exhibits reacting groups (radiate-hardening groups) developed under the effect of actinic radiation with ethylenic unsaturated compounds polymerization) and optionally further compounds (IV) with NCO reactive groups optionally in presence of catalyst: urethanes containing NCO group, which are formed with radiation hardening groups and subsequently added without other isocyanate group containing compounds and in presence of a allophanating catalyst, where the proportion of NCO groups of (II) to the OH groups of (III) and optionally (IV) is 1.45:1 to 1.1:1. Independent claims are also included for: (1) a radiation hardening allophanate (I) obtained by the method; (2) coating agents (V) comprising: one or more (I); optionally one or more polyisocyanates (having free or blocked isocyanate groups), which are free from reaction groups (developed under effect of actinic radiation with ethylenic unsaturated compounds under polymerization); optionally other compounds, which are different from (I) (which exhibit reacting groups and free or blocked NCO groups (optionally under actinizing radiation effect with ethylenic unsaturated compounds under polymerization)), optionally one or more compounds containing active hydrogen (reacting with isocyanates), initiators, optionally solvents, auxiliary materials and additives; and (3) substrates coated with the coatings obtained using (I).

DEFOAMER AND METHOD FOR THEIR PRODUCTION

Process for the preparation of polyisocyanates with a biuret structure

The present invention relates to an improved process for the preparation of polyisocyanates with a biuret structure by continuous reaction of excess amounts of organic diisocyanates having exclusively aliphatically and/or cycloaliphatically bonded isocyanate groups with organic diamines having exclusively aliphatically and/or cycloaliphatically bonded primary amino groups at elevated temperatures by 2-stage addition of the isocyanate component.

Spruehgetrocknetes Mittel fuer die Textilveredlung

Process and device for the production of (cyclo) aliphatic biuret group-containing polyisocyanants

A process and device are disclosed for preparing (cyclo)aliphatic biuret groups-containing polyisocyanates from (cyclo)aliphatic diisocyanates and steam or a dehydrating substance as reactives that are mixed with each other in a stirring reactor. The reactives flow in opposite current through a cascade-shaped stirring reactor with at least two stages. The distribution of the gaseous reactives in the liquid reactives is intensified by turbulence-generating means built into the stirring reactor. Mutually spaced disks provided with central openings and/or turbulence-generating strips that extend in the longitudinal direction of the stirring reactor are used as turbulence-generating means.

负载钌铜双金属催化剂的制备方法及其产品和应用

本发明公开一种负载钌铜双金属催化剂的制备方法及其产品和应用。该催化剂以氧化锌、氧化铝或者氧化锌和氧化铝的复合氧化物为载体，以钌铜双金属为活性组分，采用共还原铜锌、铜铝或者铜锌铝负载的钌催化剂得到。其中钌的质量分数为1%‑5%，铜的摩尔含量为30%，其他金属总摩尔含量为70%，且当其他金属为锌铝时，限制锌：铝摩尔比为1:6到6:1。该催化剂可应用在二氧化碳与胺的甲酰化反应中，提高了产物的得率。

레올로지 변형에 사용되는 혼화물

본 발명은 60 ℃ 이상의 온도(T cur )에서 경화될 조성물내 새깅 조절제(SCA)로서 사용되는 혼화물의 용도에 관한 것으로서, 상기 조성물은 결합제 및 혼화물을 포함하며, 상기 혼화물은: (a) 의도된 경화 온도보다 10 ℃ 이상 낮은 용융 온도(T m1 )를 가지므로, 요건 T m1 < (T cur - 10 ℃)를 만족시키는 틱소트로피-유발 입자체 폴리우레아 생성물; 및 (b) 상기 경화 온도 이하의 온도에서 입자 특성을 유지하는 제2 틱소트로피-유발 입자체 성분을 포함하는 것을 특징으로 한다.

Optic isomers of (+) and (-)-benzhydrylureas and (+) and (-)-1-[(3-chlorophenyl)-phenyl-methyl]urea, pharmaceutical composition based on thereof and method of thereof obtaining

FIELD: chemistry. SUBSTANCE: invention relates to optic isomers of (+)- and (-)-1-[(3- chlorophenyl)-phenyl-methyl]urea, to based on them pharmaceutical composition, possessing anti- convulsive activity, as well as to method of obtaining said isomers. Method is realized by interaction of racemic mixture of respective benzhydrylamine with tartaric acids in organic solvent with obtaining diastereomers of benzhydrylamine tartrates, which further react with cyanates of alkali metals in water solution with obtaining isomers (+)- and (-)-1-[(3-chlorophenyl)-phenyl-methyl]urea. EFFECT: optic isomers, possessing different strength of therapeutic activity and method of their obtaining. 10 cl, 1 dwg, 4 tbl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 275/18 C07C 273/02 A61K 31/17 A61P 25/08 (13) 2 537 361 C1 (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013133610/04, 18.07.2013 (24) Дата начала отсчета срока действия патента: 18.07.2013 (45) Опубликовано: 10.01.2015 Бюл. № 1 2 5 3 7 3 6 1 Адрес для переписки: 634050, г.Томск, а/я 86, ООО "АИС-БП", директору, патентному поверенному РФ (рег. N193) Бутенко Людмиле Васильевне C 1 R U оптических изомеров бензгидролов и бензгидрилмочевин, Тезисы VII Всероссийской научно-практической конференции студентов и аспирантов "Химия и химическая технология в XXI веке", Томск, 11-12 мая 2006, с.73. Umadevi, P. et al., Synthesis and in vitro antibacterial activity of some new urea, thiourea and thiosemicarbazide (см. прод.) 2 5 3 7 3 6 1 C 1 (56) Список документов, цитированных в отчете о поиске: ДУБИНИНА А.А., Получение (73) Патентообладатель(и): Общество с ограниченной ответственностью "СИНТЕГАЛ" (RU) R U Приоритет(ы): (22) Дата подачи заявки: 18.07.2013 (72) Автор(ы): Худолей Владимир Николаевич (RU), Дорошенко Александр Сергеевич (RU), Филимонов Виктор Дмитриевич (RU), Штрыкова Виктория Викторовна (RU), Куксенок Вера Юрьевна (RU) ...

Method for 1,1,3,3-tetrakis(2-hydroxyethyl)urea preparation

FIELD: chemistry. SUBSTANCE: method comprises urea reaction with ethylene carbonate at urea and ethylene carbonate molar ratio of 1:4, respectively, in the presence of synthetic zeolites containing 0.4-0.9 wt % of sodium oxide or 0.4-0.9 wt % of sodium oxide and 1.0-5.5 wt % of potassium oxide in its composition. The process is conducted at a temperature of 140-150°C until carbon dioxide emission stops. EFFECT: invention allows to increase compound yield and reduce production time. 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 619 586 C1 (51) МПК C07C 273/18 (2006.01) C07C 275/10 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2016103237, 01.02.2016 (24) Дата начала отсчета срока действия патента: 01.02.2016 Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 01.02.2016 (45) Опубликовано: 17.05.2017 Бюл. № 14 (56) Список документов, цитированных в отчете о поиске: US 5858549 A1, 12.01.1999. JP 6293727 A, 21.10.1994. US 20110105654 A1, 05.05.2011. SU 176578 A1, 17.11.1965. CN 103012211 A, 03.04.2013. 2 6 1 9 5 8 6 R U (57) Формула изобретения Способ получения 1,1,3,3-тетракис(2-гидроксиэтил)мочевины путем взаимодействия мочевины с этиленкарбонатом в мольном соотношении мочевины и этиленкарбоната 1:4 соответственно в присутствии синтетических цеолитов, содержащих в своем составе оксид натрия в количестве 0.4-0.9 мас. % или оксид натрия в количестве 0.4-0.9 мас. % и оксид калия в количестве 1.0-5.5 мас. %, процесс ведут при температуре 140-150°C до окончания выделения двуокиси углерода. Стр.: 1 C 1 C 1 (54) Способ получения 1,1,3,3-тетракис(2-гидроксиэтил)мочевины 2 6 1 9 5 8 6 Адрес для переписки: 420015, Татарстан, г. Казань, ул. К. Маркса, 68, ФГБОУ ВО "КНИТУ", отдел патентноизобретательской деятельности (73) Патентообладатель(и): Федеральное государственное бюджетное образовательное учреждение высшего образования "Казанский национальный исследовательский технологический ...

具有末端脲和/或氨基甲酸酯基团的新型碳二亚胺、用于生产所述碳二亚胺的方法、以及所述碳亚二胺的用途

本发明涉及新型的具有式(I)的碳二亚胺，这些碳二亚胺具有末端脲和/或氨基甲酸酯基团，其中R可以是相同的或不同的并且选自-NHCONHRˊ、-NHCONRˊR”和-NHCOOR”ˊ残基的组。本发明进一步涉及用于生产所述碳二亚胺的方法，以及所述碳二亚胺在以下各项中作为稳定剂的用途：基于酯的多元醇、聚对苯二甲酸乙二酯(PET)、聚对苯二甲酸丁二酯(PBT)、聚对苯二甲酸丙二酯(PTT)、共聚酯、热塑性聚酯弹性体(TPE-E)、乙烯乙酸乙烯酯(EVA)、聚乳酸(PLA)和/或PLA衍生物、聚对苯二甲酸己二酸丁二酯(PBAT)、聚琥珀酸丁二酯(PBS)、多羟基烷酸酯(PHA)、共混物、甘油三酯、热塑性聚氨酯、聚氨酯弹性体、PU粘合剂、PU铸模树脂、PU涂料或PU泡沫。

Process and device for preparing (cyclo)aliphatic biuret groups-containing polyisocyanates

In a process and an apparatus for preparing (cyclo)aliphatic polyisocyanates containing biuret groups from (cyclo)aliphatic diisocyanates and steam or a substance capable of splitting off water as reactants which are mixed with one another in a stirred reactor, the reactants are passes in countercurrent through a cascade-type stirred reactor comprising at least two stages. The dispersion of the gaseous reactant in the liquid reactant is reinforced by baffles installed in the stirred reactor. As baffles, use is made of discs provided with central openings and arranged at a distance from one another and/or strip baffles running in the longitudinal direction of the stirred reactor.

Method for separating water from a mixture containing water, carbon dioxide and amine

用于粘合剂树脂的交联组分

本发明涉及用于粘合剂树脂的交联组分，所述交联组分特别适合与包含环氧基的粘合剂和/或(多)异氰酸酯例如封端(多)异氰酸酯一起使用，并且所述交联组分的每个分子包含至少两个封端异氰酸酯基团，其中至少两个封端异氰酸酯基团中的至少一者为根据结构单元(I)的基团，其中式(II)的结构单元(如果存在的话)与式(I)的结构单元之比为0.40或更小。所述交联组分也可以是可自交联的。本发明还涉及涂料组合物，例如包含所述交联组分的单组分涂料组合物，及其制备方法。

Process for preparing higher ethylene amines

Process to prepare higher ethylene amines and ethylene amine derivatives

The present invention relates to a process to prepare ethylene amines of the formula NH 2 -(C 2 H 4 -NH-) p H wherein p is at least 3 or derivatives thereof wherein one or more units -NH-C 2 H 4 -NH- may be present as a cyclic ethylene urea unit or between two units -NH-C 2 H 4 -NH- a carbonyl moiety is present, by reacting an ethanolamine-functional compound, an amine-functional compound in the presence of a carbon oxide delivering agent, wherein the molar ratio of carbon oxide delivering agent to amine-functional compound is at least 0.6 to 1.

Polymers with upper critical dissolution temperature in aqueous solution

양태는 일반적으로 온도 반응성 중합체, 보다 구체적으로 수용액에서 상부 임계 용해 온도(UCST)를 나타내는 중합체에 관한 것이다. 일 양태에서, 단량체 화합물은 하나 이상의 아미드 또는 티오아미드 기; 하나 이상의 우레이도 또는 티오우레이도 기; 및 하나 이상의 에틸렌계 불포화기를 포함한다. 일 양태에서, 동종중합체 또는 공중합체와 같은 중합체는 단량체 화합물의 중합에 의해 생성된다. 공중합체는 소수성 공단량체, 친수성 공단량체, pH 반응성 공단량체, 광반응성 공단량체 및 이들의 조합과 같은 단량체 화합물 및 공단량체의 중합에 의하여 생성된다. 중합체는 1 atm에서 수용액에서 약 1℃ 내지 약 100℃의 UCST를 나타낸다.

Method of obtaining n-substituted trichloracetamidines or salts thereof

Process and Device for Preparing (Cyclo)Aliphatic Biuret Groups-Containing Polyisocyanates

교반 반응기 내에서 서로 혼합되는 반응물로서 (시클로)지방족 디이소시아네이트 및 스팀 또는 물을 분리할 수 있는 물질로부터 비우레트기 함유 (시클로)지방족 폴리이소시아네이트를 제조하는 방법 및 장치에서, 반응물은 2단계 이상으로 이루어지는 케스케이드형 교반 반응기를 통하여 반대방향으로 통과된다. 기상 반응물의 분산은 교반 반응기에 설치된 배플에 의해 강화된다. 배플로서는 중앙 개구부를 갖고 서로 간격을 두고 배치된 디스크 및(또는) 교반 반응기의 종방향으로 뻗어있는 스트립 배플을 이용한다. In a method and apparatus for producing a (cyclo) aliphatic polyisocyanate from a (cyclo) aliphatic diisocyanate and a substance capable of separating steam or water as a reactant to be mixed with each other in a stirring reactor, Lt; RTI ID = 0.0 &gt; cascade &lt; / RTI &gt; The dispersion of the gaseous reactants is enhanced by the baffles installed in the stirred reactor. The baffles utilize longitudinally extending strip baffles of discs and / or agitating reactors having a central opening and spaced apart from each other.

Method for 1,3-bis(2-hydroxyethyl)urea production

FIELD: chemistry. SUBSTANCE: method comprises urea reaction with ethylene carbonate at urea and ethylene carbonate molar ratio of 1:2, respectively, in the presence of synthetic zeolites containing 0.4-0.9 wt % of sodium oxide or 0.4-0.9 wt % of sodium oxide and 1.0-5.5 wt % of potassium oxide in its composition. The process is conducted at a temperature of 140-150°C until carbon dioxide emission stops. EFFECT: invention allows to increase compound yield and reduce production time. 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 619 588 C1 (51) МПК C07C 273/18 (2006.01) C07C 275/10 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2016103278, 01.02.2016 (24) Дата начала отсчета срока действия патента: 01.02.2016 Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 01.02.2016 (45) Опубликовано: 17.05.2017 Бюл. № 14 (56) Список документов, цитированных в отчете о поиске: US 5858549 A1, 12.01.1999. JP 6293727 A, 21.10.1994. US 20110105654 A1 (DICKE R. et al), 05.05.2011. SU 176578 A1, 17.11.1965. CN 103012211 A, 03.04.2013. 2 6 1 9 5 8 8 R U (57) Формула изобретения Способ получения 1,3-бис(2-гидроксиэтил)мочевины путем взаимодействия мочевины с этиленкарбонатом в мольном соотношении мочевины и этиленкарбоната 1:2, соответственно, в присутствии синтетических цеолитов, содержащих в своем составе оксид натрия в количестве 0.4-0.9 мас. % или оксид натрия в количестве 0.4-0.9 мас. % и оксид калия в количестве 1.0-5.5 мас. %, процесс ведут при температуре 140-150°C до окончания выделения двуокиси углерода. Стр.: 1 C 1 C 1 (54) Способ получения 1,3-бис(2-гидроксиэтил)мочевины 2 6 1 9 5 8 8 Адрес для переписки: 420015, Татарстан, г. Казань, ул. К. Маркса, 68, ФГБОУ ВО "КНИТУ", отдел патентноизобретательской деятельности (73) Патентообладатель(и): Федеральное государственное бюджетное образовательное учреждение высшего образования "Казанский национальный исследовательский технологический ...

Process for producing polyisocyanates containing biuret groups from (cyclo) aliphatic diisocyanates

A process is disclosed for producing a polyisocyanate containing biuret groups from at least one aliphatic, cycloaliphatic or araliphatic diisocyanate or a mixture of two or more such substances, and from at least one amine or water or a mixture of water and at least one amine as reactants. The reactants are mixed together and made to react in a mixing element with a high shearing effect.

Process for the preparation of 1,5 naphtylene diisocyanate having urea and biuret groups

Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von Harnstoff- und Biuretgruppen enthaltendem 1,5-Naphthylendiisocyanat, wobei 1,5-Naphthylendiisocyanat mit 0,02 bis 0,5, vorzugsweise 0,1 bis 0,25 Mol Wasser pro Mol Isocyanat in Abmischung mit der 1- bis 10-fachen, vorzugsweise 2- bis 5-fachen Menge, berechnet pro Gewichtseinheit Wasser, eines organischen Lösungsmittels umgesetzt wird. The present invention relates to a process for the preparation of 1,5-naphthylene diisocyanate containing urea and biuret groups, 1,5-naphthylene diisocyanate mixed with 0.02 to 0.5, preferably 0.1 to 0.25, mol of water per mol of isocyanate is reacted with 1 to 10 times, preferably 2 to 5 times the amount, calculated per unit weight of water, of an organic solvent.

Compounds containing aldimine

The invention relates to compounds of formula (I) which contain aldimine, and to the use thereof. Said compounds which contain aldimines are characterised in that they are odour-less and during hydrolysis the odour-free aldehydes are separated. They are used, therefor, as sources for aldehydes. They can also be used in cross-linking reactions.

Frocess for producing amino salts of substituted n-phosphonomethyl ureas

Nolvel amine salts of substituted phosphonomethylureas having the formula in which R,R' and R" are independently C 1 -C 4 alkyl; a is 1 or2 and b is2 or3, such thatthe sum of a and b is4; and c is 1 or 2 and d is 0 or 1, such that the sum of c and d is 2. These compounds are useful in regulating the natural growth or development of plants. They may be prepared by reacting the appropriate amine ReNHtb, where b' is 1 or2, with an appropriate phosphonic acid. A rate of application of 0.11 to 22 kg/ ha is suitable. For application the compounds may be formulated with an inert carrier or diluent A preferred compound is the mono(diisopropylamine) salt of N,N-dimethyl- N-carboethoxymethyl-N'-phosphonomethylurea.

Method for synthesizing O-methyl isourea hydrogen sulfate

本发明公开了一种合成O‑甲基异脲硫酸氢盐的方法，属于有机合成技术领域。本发明采用在超声波反应釜中进行甲基化反应，将超声波发生器按照特定频率间歇性工作，缩短反应时间，降低了反应的温度，提高了产物得率。本专利所涉及的甲基化反应采用超声波反应釜进行，是一种安全环保的绿色合成新技术。

Method of obtaining phloroglucinol

Glycogen Phosphorylase Inhibitor Compounds and Pharmaceutical Compositions Thereof

The invention relates to glycogen phosphorylase inhibitor compounds, pharmaceutical compositions of these compounds, methods of treatment using the pharmaceutical compositions to treat diabetes, conditions associated with diabetes, and/or tissue ischemia, including myocardial ischemia, and processes for making the compounds.

Glycogen phosphorylase inhibitor compounds and pharmaceutical compositions thereof

(miscellaneous) aryl cyclopropyl amines as LSD1 inhibitor

本发明涉及(杂)芳基环丙基胺化合物，特别包括如本文所述和所定义的式I的化合物，且本发明涉及它们在疗法中的用途，包括例如在治疗或预防癌症、神经系统疾病或病症或病毒感染中的用途。