СПОСОБ ПОЛУЧЕНИЯ ФТОРАЛКИЛСОДЕРЖАЩИХ α,β-НЕПРЕДЕЛЬНЫХ КЕТОНОВ

Способ получения фторалкилсодержащих α, β-непредельных кетонов общей формулы RF - CH = CHCOR, где RF= X(CF2)m; X = H, F; m = 1-6; R = (CH3)3C; C6H5, путем взаимодействия соответствующего гидрата фторированного альдегида с метилкетоном в присутствии конденсирующего и дегидратирующего агента, отличающийся тем, что, с целью увеличения выхода целевого продукта и упрощения процесса, в качестве конденсирующего и дегидратирующего агента используют полифторкарбоновую кислоту H(CF2)nCOOH, где n = 1-4, или смесь полифторкарбоновых кислот, являющихся кубовыми остатками электрохимического производства трифторуксусной кислоты при молярном соотношении гидрата фторированного альдегида и полифторкарбоновой кислоты 1:1-3.

Verfahren zur Herstellung von Benzylketonen.

TRIARYLMETHANVERBINDUNGEN ZUR BEHANDLUNG VON KREBS, AKTINISCHER KERATOSE UND KAPOSISARKOM

Chemical compounds

... 4-(6-Substituted naphthyl)butan-2-ols,-butan-2-ones,-pentan-2-ols and -pentan-2-ones bearing a fluoro group in the naphthyl ring, and pro-drugs thereof, are anti-inflammatory agents. A typical embodiment is 4-(4-fluoro-6-methoxy-2-naphthyl)-butan-2-one.

VERFAHREN ZUR HERSTELLUNG VON RACEMISCHEN PHENYLALKYLAMINEN

TETRAHYDRO NAPHTALINDERVIATE ONE AS GLUCOCORTICOIDREZEPTOR MODULATORS

PROCEDURE FOR THE PRODUCTION OF HALOGENIERTEN CONNECTIONS

MANUFACTURING PROCESS OF TRI FLUORINE METHYL CONNECTIONS.

PROCEDURE FOR THE PRODUCTION OF RACEMI PHENYLALKYLAMINEN

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

11, DEOXY PGE DERIVATIVES

Retroviral protease inhibiting compounds

PROCESS FOR PREPARING HALOGENATED COMPOUNDS

PROCESS FOR RECOVERING PHENYLALKYLAMINES

HYDROXYETHYL-AZOLE COMPOUNDS, THEIR PRODUCTION AND THEIR MEDICINAL USE

The invention relates to hydroxyethyl-azole compounds and methods for their preparation. The compounds are useful pharmacologically as antimycotic agents. They correspond to the general formula (I) in which Az denotes an imidazole or triazole radical, R represents phenyl optionally mono or di-substituted by chlorine, fluorine or methyl, or represents naphthyl or tetrahydronaphthyl, R1 represents phenyl or cycloalkyl optionally substituted by chlorine, bromine, fluorine, alkyl with 1 to 4 carbon atoms, or alkoxy with 1 to 4 carbon atoms, R2 represents hydrogen, or R1 and R2 together, in the o-position relative to one another, represent a polymethylene bridge optionally substituted by chlorine or methyl, or, together with the phenyl ring, represent naphthyl, R3 denotes a halogen atom or an alkyl, alkoxy or halogeno-alkyl group and n is 0, 1, 2 or 3.

CURCUMIN ANALOGUES FOR TREATING CANCER

The present invention is directed to curcumin analogs (I), wherein Y is OH, halogen, or CF3; Z is H, OH, OR1, halogen, or CF3; X1 and X2 are independently C or N; and A is as defined in the application; exhibiting anti-tumor and anti- angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.

C2-PHENYL-SUBSTITUTED CYCLIC KETO-ENOLS AS PESTICIDES AND HERBICIDES

... ²²The present invention relates to novel C2-phenyl-substituted cyclic ketoenols ²of the ²formula (I)²(see formula I)² in which²W, X, Y, Z and CKE are as defined in the description, to processes for their ²preparation and to their use as pesticides and herbicides.² ...

4-CHLORO-4-ALKOXY-1,1,1-TRIFLUORO-2-BUTANONES, THEIR PREPARATION AND THEIR USE IN PREPARING 4-ALKOXY-1,1,1-TRIFLUORO-3-BUTEN-2-ONES

... 4-Chloro-4-alkoxy-1,1,1-trifluoro-2-butanones, prepared by reacting alkyl vinyl ethers with trifluoroacetyl chloride, are useful for preparing 4-alkoxy- 1,1,1-trifluoro-3- buten-2-ones.

NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES

Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.

DIPHENYL-2-PROPENOATES AND HOMOLOGS THEREOF USEFUL FOR TREATING DISEASES ASSOCIATED WITH LEUKOTRIENE B4

This invention relates to a compound of formula (I), where the several groups are defined herein. These compounds are leukotriene antagonists an as such can be used in treating various diseases associated with leucotrienes.

Verfahren zur Herstellung von alkylierten Arylmethyl-methylketonen.

Process for the preparation of new cyclopentane derivatives

The derivatives of the cyclopentane of formula below are prepared by hydrolysis of a corresponding 5-ketal. In this formula, R<2> = aryl or heterocyclyl, n = 5 to 8, and: either A = alkylene, X = trans vinylene or ethylene, Y = carbonyl or hydroxymethylene and Z = direct bond or O or S atom, or A and Z = direct bonds, and X and Y are respectively ethylene and carbonyl, trans vinylene and carbonyl, or ethylene and hydroxymethylene. These compounds are active in particular against gastric acid secretion and for the cicatrisation of gastric ulcers. ...

5-[(3,3,3-ТРИФТОР-2-ГИДРОКСИ-1-АРИЛПРОПИЛ)АМИНО]-1H-ХИНОЛИН-2-ОНЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНЫХ СРЕДСТВ

Настоящее изобретение относится к соединениям формулы I способам их получения и их применению в качестве противовоспалительных средств.

is 5th [(3,3,3-TRIFLUORO-2- HYDROXy -1-[ARILPROPIL]) AMINO] - 1H- QUINOLINE -2-[ONY], THE METHOD OF THEIR OBTAINING and THEIR APPLICATION AS THE ANTIPYRETIC MEANS

5-[(3,3,3-ТРИФТОРО-2-ГИДРОКСИ-1-АРИЛПРОПИЛ)-АМИНО]-1H-ХИНОЛИН-2-ОНЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНЫХ СРЕДСТВ

Данное изобретение касается соединений формулы I , (I) способов их получение и их применения в качестве противовоспалительных средств.

B-DICETONES SUBSTITUEES, LEUR PREPARATION ET LEUR UTILISATION COMME AGENTS ANTI-VIRAUX

L'invention concerne des beta -dicétones substituées sur l'atome de carbone compris entre les deux groupements carbonyle par un groupement aryle aliphatique dont la chaîne aliphatique est interrompue par un groupement cyclique (phényle éventuellement substitué, cyclohexyle ou furyle), que l'on prépare en faisant réagir l'halogénure aryl-aliphatique approprié avec un sel de métal alcalin d'une beta -dicétone. Les composés ainsi obtenus ont une activité antivirale.

Procédé de préparation de dérivés du biphényle.

L'invention concerne la préparation de dérivés du biphényle de formule : ...

NEW DERIVATIVES OF CYCLOPENTANE

Racemising 1-phenyl-2-aminopropanes - by oxidising to ketone with N-chloro succinimide then reaction with amine

불소 함유 착체 화합물, 및 이것을 사용하는 불소 함유 유기 화합물의 제조 방법

... 본 발명은 여러가지, 테트라플루오로에틸렌 구조(-CF2-CF2-)의 양쪽 말단에 유기기를 갖는 불소 함유 화합물의 합성을 가능하게 하는 것을 목적으로 한다. 본 발명은 식 (1a): [식 중, M1은, 구리, 아연, 니켈, 철, 코발트 및 주석으로 이루어지는 군에서 선택되는 금속을 나타내고; R1은, 유기기를 나타낸다.] 으로 표시되는 불소 함유 유기 금속 화합물, 및 피리딘환을 갖는 화합물, 및 포스핀으로 이루어지는 군에서 선택되는 배위자 를 포함하는 불소 함유 착체 화합물을 제공한다.

BETASUBSTITUERADE DIKETONER OCH FORFARANDE FOR FRAMSTELLNING DERAV

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

СПОСОБ ПОЛУЧЕНИЯ ФТОРМЕТИЛПРОИЗВОДНОГО

Способ получения производных бензилтрифторметилкетона

Изобретение касается замещенных кетонов, в частности получения производных бензилтрифторметилкетона общей ф-лы X - C6H4- CH2C(O) - CF3, где X = H, 4-F, 4-CH3, 3,4-ди-CL -полупродуктов для синтеза термостойких полимеров. Цель - расширение ассортимента целевых веществ, упрощение и интенсификация процесса. Его ведут реакцией диэтиламида трифторуксусной кислоты с бензилмагнийхлоридом или бензилмагнийбромидом при 0-40°С в среде эфира с последующим гидролизом магний-органического производного. Эти условия сокращают время процесса с 40-50 до 11-13 ч при использовании простых и доступных реагентов с достижением 56-75%-ного выхода целевых веществ. 1 табл.

TRIARYLMETHANVERBINDUNGEN ZUR BEHANDLUNG VON KREBS, AKTINISCHER KERATOSE UND KAPOSISARKOM

Compounds

CHEMICAL COMPOUNDS

ARYLVINYL CYCLOPROPYL KETONES

... 1414569 Aryl vinyl cyclopropyl ketones STERLING DRUG Inc 18 June 1973 [22 June 1972] 33859/74 Divided out of 1414568 Heading C2C The invention comprises aryl vinyl cyclopropyl ketones of the formula wherein R is hydrogen or lower alkyl of 1 to 4 carbon atoms, and Ar is phenyl, naphthyl or phenyl substituted by 3, 4 methylenedioxy or from one to three lower alkyls of 1 to 4 carbon atoms, lower alkoxy of 1 to 4 carbon atoms, carbo-lower alkoxy of 2 to 4 carbon atoms, halogen, trifluoromethyl, trifluoromethoxy, hydroxy, benzyloxy, alkanoylamino of 1 to 4 carbon atoms or dialkylamino (where alkyl has from 1 to 4 carbon atoms) radicals. The aryl vinyl cyclopropyl ketones may be prepared by reacting 1-R-1-acetyl cyclopropane with an aldehyde of the formula Ar-CHO in the presence of a base.

Organic compounds

USE TRIFLUORINE ACETYL ALKYL SUBSTITUTE PHENYL- ONE, PHENOL AND BENZOYLDERIVATE IN THE TREATMENT AND/OR PROPHYLAXIS OF OBESITAS AND THEIR BEGLEIT AND/OR SUBSEQUENT ILLNESSES

TRI ARYL METHANE CONNECTIONS TO THE TREATMENT OF CANCER, AKTINI KERATOSE AND KAPOSISARKOM

HISTONE DEACETYLASE INHIBITORS BASED ON TRIHALOMETHYLCARBONYL COMPOUNDS

Use of trifluoroacetyl alkyl-substituted phenyl derivatives, phenol derivatives and benzoyl derivatives in the treatment and/or prophylaxis of obesity and accompanying diseases and/or secondary diseases

CHEMICAL COMPOUNDS

DIKETONES, KETO-ESTERS AND THEIR PREPARATION

Aryl substituted diketones and keto-esters having the Formula I (herein), useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester.

ARALIPHATIC KETONES AND SECONDARY ALCOHOLS

DERIVES DU NAPHTALENE UTILISABLES COMME MEDICAMENT

CETTE INVENTION CONCERNE DE NOUVEAUX DERIVES DU NAPHTALENE. ELLE CONCERNE PLUS SPECIALEMENT UN COMPOSE DE FORMULE: (CF DESSIN DANS BOPI) (CF DESSIN DANS BOPI) OU UN COMPOSE DONNANT NAISSANCE A CE COMPOSE DANS L'ORGANISME, FORMULE DANS LAQUELLE R EST UN ATOME D'HYDROGENE OU UN GROUPE METHYLE, X EST UN GROUPE CO OU CHOH, Y EST UN ATOME DE CHLORE OU DE BROME OU BIEN UN GROUPE ALCOYLE EN C, METHOXY OU METHYLTHIO, LA LIGNE EN POINTILLE REPRESENTE UNE DOUBLE LIAISON EVENTUELLEMENT PRESENTE, ET F EST UN ATOME DE FLUOR EN POSITION 1 A4. CES COMPOSES CONSTITUENT EN PARTICULIER DES AGENTS ANTI-INFLAMMATOIRES.

DERIVED FROM NAPHTHALENE USABLE LIKE DRUG

PROCEDE POUR LA PREPARATION DES CARBINOLES ARALIPHATIQUES

PERFLUOROKETONE COMPOUNDS AND USES THEREOF

Novel perfluoroketone compounds of formula [I] and [Ia] are described Also described are uses thereof, such as for inhibition of phospholipase A2 activity. Therapeutic uses thereof are also described, such as for the treatment of neural conditions and / or inflammatory conditions, such as demeyelmatmg (e.g., multiple sclerosis) and neural injury (e.g., spinal cord injury).

Substituted 5-cycloalkyl-2,2-dimethyl-pentan-3-one

Novel substituted 5-cycloalkyl-2,2-dimethyl-pentan-3-ones of the formula (I) in which R is optionally substituted cycloalkyl, X is halogen and Y is hydrogen or halogen, The new compounds are valuable intermediates for the synthesis of substances having plant growth-regulating and fungicidal properties.

SEMICONDUCTOR MANUFACTURING EQUIPMENT

PURPOSE: To improve the throughput of a single wafer semiconductor manufacturing equipment while restraining the equipment cost, which is equipped with the atmosphere side load lock chamber delivering wafers to a carrier cassette in the atmosphere and a reaction chamber side load lock chamber including a vacuum transfer robbot. CONSTITUTION: The title equipment is constituted by using the atmosphere side load lock chamber 101 accommodating a wafer stage on which wafers before and after treatment are mounted, and a first and a second load lock chambers which include the respective vacuum transfer robbots 5. The wafers circulate in the order through the atmosphere side load lock chamber, the first load lock chamber, a reaction chamber, the second load lock chamber and the atmosphere side load lock chamber. The wafers before treatment can always be kept waiting in the first load lock chamber. Time necessary to evacuate the inside of the atmosphere side load lock chamber as required in the ...

ФЕНФЛУРАМИНОВЫЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ

Изобретение относится к способу получения фенфлураминового активного фармацевтического ингредиента. Предлагаемый способ включает стадии (a)-(e). На стадии (a) осуществляют гидролиз 2-(3-(трифторметил)фенил)ацетонитрильной композиции с получением композиции 2-(3-(трифторметил)фенил)уксусной кислоты. На стадии (b) производят очистку композиции 2-(3-(трифторметил)фенил)уксусной кислоты с получением очищенной композиции 2-(3-(трифторметил)фенил)уксусной кислоты. На стадии (c) очищенная композиция 2-(3-(трифторметил)фенил)уксусной кислоты взаимодействует с уксусным ангидридом и катализатором с получением композиции 1-(3-(трифторметил)фенил)пропан-2-она. На стадии (d) осуществляют очистку композиции 1-(3-(трифторметил)фенил)пропан-2-она с использованием кетонового бисульфитного аддукта с получением очищенной композиции 1-(3-(трифторметил)фенил)пропан-2-она. На стадии (e) производят восстановительное аминирование композиции 1-(3-(трифторметил)фенил)пропан-2-она этиламином с использованием боргидридного ...

СПОСОБ ПОЛУЧЕНИЯ 4,4-ДИМЕТИЛ-1-(П-ХЛОРФЕНИЛ)-ПЕНТАН-3-ОНА

Изобретение относится к способу получения 4,4-диметил-1-(п-хлорфенил)пентан-3-она, который является промежуточным продуктом для получения пестицидов и фармацевтических продуктов, в том числе тебуконазола. Способ заключается в конденсации пинаколина с п-хлорбензальдегидом в среде водного бутилового спирта в присутствии щелочи и проведении процесса гидрирования в расплаве полученного 4,4-диметил-1(п-хлорфенил)пент-1-ен-3она в присутствии катализатора Ni-Re. Способ позволяет проводить процесс гидрирования с большей скоростью и при меньшем расходе катализатора, снизить образование побочных продуктов. 3 з.п. ф-лы, 1 табл.

BETA-SUBSTITUTED-DIKETONES AND PREPARATION THEREOF

TRI FLUORINE BENZENE DERIVATIVES AND IT ABSTENTION LIQUID CRYSTAL COMPOSITIONS.

HYDROXYETHYL AZOLE, PROCEDURE FOR YOUR PRODUCTION AS WELL AS YOUR USE AS DRUGS.

RETROVIRALPROTEASEHEMMENDE CONNECTIONS

INTERMEDIATE PRODUCTS FOR THE PRODUCTION OF NON PEPTIDEN RETROVIRALPROTEASEHEMMENDEN CONNECTIONS

PYRIDAZINVERBINDUNG AND THEIR USE

Diphenyl-2-propenoates and homologs thereof useful for treating diseases associated with leukotriene b4

GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate,or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

PROCESS FOR THE PREPARATION OF METHYL KETONES

BETA-SUBSTITUTED-DIKETONES AND PREPARATION THEREOF

4-CHLORO-4-ALKOXY-1,1,1-TRIFLUORO-2-BUTANONES, THEIR PREPARATION AND THEIR USE IN PREPARING 4-ALKOXY-1,1,1-TRIFLUORO-3-BUTEN-2-ONES

... 4-Chloro-4-alkoxy-1,1,1-trifluoro-2-butanones, prepared by reacting alkyl vinyl ethers with trifluoroacetyl chloride, are useful for preparing 4-alkoxy-1,1,1-trifluoro-3- buten-2-ones.

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A retroviral protease inhibiting compound of the formula A-X-B or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group; A is (1) substituted amino, (2) substituted carbonyl, (3) functionalized imino, (4) functionalized alkyl, (5) functionalized acyl, (6) functionalized heterocyclic or (7) functionalized (heterocyclic)alkyl; and B is (1) substituted carbonyl independently defined as herein, (2) substituted amino independently defined as herein, -332- (3) functionalized imino independently defined as herein, (4) functionalized alkyl independently defined as herein, (5) functionalized acyl independently defined as herein, (6) functionalized heterocyclic independently defined as herein or (7) functionalized (heterocyclic)alkyl independently defined as herein.

HYDRAZONE COMPOUNDS, PROCESSES FOR THEIR PRODUCTION, INTERMEDIATES USEFUL FOR THEIR PRODUCTION AND PESTICIDAL COMPOSITIONS CONTAINING THEM

The present invention relates to a hydrazone compound of the formula (I) or its salt, a process for its preparation, an intermediate of the formula (II-5), a pesticidal composition containing said hydrazone compound or its salt as the active ingredient, and a pesticidal method of applying an effective amount thereof: (I) (II-5) ...

METHOD OF PREPARATION OF DERIVED FROM BIPHENYL

CHEMICAL COMPOUNDS

Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11βHSD1 are described. © KIPO & WIPO 2007 ...

COMPOSITION OR a PHARMACEUTICAL ACCEPTABLE SALT OF This, USE OF The same, PHARMACEUTICAL COMPOSITION, and, METHOD TO PRODUCE an INHIBITING EFFECT OF 11BETAHSD1 IN an ANIMAL OF HOT BLOOD, AS the MAN, IN NECESSITY OF SUCH TREATMENT

PROCESS FOR THE PREPARATION OF ILOPERIDONE USING A NOVEL INTERMEDIATE

The present invention provides a novel process for the preparation of iloperidone using a novel intermediate. Thus for example, reacting 4-(3- chloropropoxy)-3-methoxy benzaldehyde with methyl magnesium iodide in ether and the reaction mass was heated for 6 hours at reflux temperature, the mass was cooled to ambient temperature and poured into a mixture of ice, water and dilute hydrochloric acid to obtain l-[4-(3-chloropropoxy)-3-methoxyphenyl]ethanol.

Alkylamino- and alkylamino alkyl diarylketones and pharmaceutical compositions thereof

This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula where Ar is aryl of the formula where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF3, NO2 and u is an integer of 1 to 3; X and Y are independently CH2+13, -CF2- or -CHF-; Z and W are independently -CH2-, -O-, -CHOH-, or -CHF-; m, n, p, q and t are integers which are independently 0 or 1, R1 is H or loweralkyl; R2 and R3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.

Novel diketones

Beta-diketones substituted by an aryl-aliphatic group in which the aliphatic chain is interrupted by a cyclic group, and useful as anti-viral agents, are prepared by interacting the appropriate aryl-aliphatic halide with an alkali metal salt of a beta-diketone.

Fatty acid amide hydrolase inhibitors

Disclosed are compounds of formula RXY that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1 and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid ...

TRIAZOLYLBUTANE DERIVATIVES WITH A FUNGICIDAL ACTION

Described are triazolylbutane derivatives of the formula (I), in which A may be a keto group or a CH(OH) grouping and R may be alkyl, optionally substituted cycloalkylalkyl, alkenyl, alkinyl or haloalkenyl (with the exception of 3-chlorobut-2-en-1-yl), as well as acid addition salts and metal-salt complexes thereof. Also described are a method of preparation of such derivatives and their use as fungicides, as well as intermediate used in the preparation, a method of preparing such intermediates and their use in the synthesis of triazolylbutane derivatives of the formula (I).

PRODUCTION OF FLUORINE-CONTAINING CARBONYL COMPOUND

PURPOSE: To produce the optically active titled compound having high optical purity, in high yield and purity, by reacting an optically active enamine with a fluorine-containing halide in the presence of a specific metal and catalyst under the action of ultrasonic wave, and treating the product with an acid. CONSTITUTION: The objective optically active fluorine-containing carbonyl compound of formula IV (* is chiral carbon atom) is produced by (1) reacting the carbonyl compound of formula I (R1 and R2 are univalent hydrocarbon group or hetero-hydrocarbon group, or together form a bivalent hydrocarbon group or hetero-hydrocarbon group forming a ring; R3 is H or hydrocarbon group) with the optically active proline derivative of formula II (R4 is hydrocarbon group), (2) reacting the resultant optically active enamine of formula III with the fluorine-containing halide of formula RfX (Rf is fluorine-containing hydrocarbon group; X is halogen) in the presence of a metal such as zinc powder and ...

СПОСОБ ПОЛУЧЕНИЯ α,β- НЕНАСЫЩЕННЫХ КЕТОНОВ

Предложен способ получения α,β - -ненасыщенных кетонов формулы RC6H4CH = CHC(O)Ar (I а-м, где R = H, 2-OH, 4-OCH3, 4-Cl, 4-Br, 2-F, 3-NO2, 4-NO2, Ar = RC6H4, конденсацией RC6H4CHO (II) и ArCOCH3 (III) в присутствии сульфированного угля. Реакцию эквимолярных количеств II и III проводят при температуре 80 - 120oС в апротонных растворителях (бензол, толуол, циклогексан) с азеотропной отгонкой воды или без растворителя в течение 0,5 - 1,0 часа. Выходы 1 85 - 96%. Пример. Смесь 0,096 молей 4-бромацетофенона и 4-нитробензальдегида, 0,05 г сульфированного угля и 10 мл циклогексана кипятили с ловушкой Дина-Старка в течение 40 мин. Осадок 4-нитро, 4′- бромхалкона в смеси с углем после охлаждения смеси отделяли, промывали метанолом и кристаллизовали из спирта. Получили 94% теор.халкона Т.пл 165 - 167oС.

СПОСОБ ПОЛУЧЕНИЯ 4,4-ДИМЕТИЛ-1-(П-ХЛОРФЕНИЛ)-ПЕНТАН-3-ОНА

... 1. Способ получения 4,4-диметил-1-(п-хлорфенил)пентан-3-она, включающий конденсацию пинаколина и п-хлорбензальдегида в присутствии щелочи в среде алифатического спирта с последующим гидрированием полученного 4,4-диметил)-1-(п-хлорфенил)пент-1-ен-3-она в присутствии катализатора Ni-Re при повышенной температуре и давлении водорода, отличающийся тем, что в качестве алифатического спирта используют водный бутиловый спирт, а процесс гидрирования проводят в расплавленном 4,4-диметил-1-(п-хлорфенил)пент-1-ен-3-оне. 2. Способ по п.1, отличающийся тем, что водный бутиловый спирт содержит 16 об.% воды. 3. Способ по п.1, отличающийся тем, что Ni-Re добавляют в количестве 0,4-1 вес.% от количества непредельного кетона. 4. Способ по п.1, отличающийся тем, что процесс гидрирования проводят при температуре 90-140°С и давлении 2-100 бар.

Способ разложения гидроперекиси в процессе получения кетона и/или спирта окислением кислородом циклического углеводорода

ARALIPHATIC KETONES AND SECONDARY ALCOHOLS

... 1497857 Araliphatic ketones and sec. alcohols DR KARL THOMAE GmbH 17 Dec 1974 [17 Dec 1973 26 Oct 1974] 54467/74 Heading C2C Novel araliphatic ketones and see. alcohols of the general formula wherein R 1 is an isobutyl group, a phenyl group optionally substituted in the 2-position by a fluorine or chlorine atom, a oyclohexyl group optionally substituted by a methyl group, or a cyclopentyl or cycloheptyl group, R 2 is a hydrogen, fluorine, chlorine or bromine atom, R 3 is a methyl or ethyl group or, when R 1 is an optionally substituted phenyl group or R 1 is a cyclohexyl group and R 2 is a halogen atom, R 3 may be a hydrogen atom, Z 1 and Z 2 are each a hydrogen atom or together form a C-C bond, A is CO or CHOH and m is 2, 4, 6 or 8 or, when R 1 is a phenyl group substituted by a fluorine or chlorine atom, an isobutyl group, a cyclohexyl group optionally substituted by a methyl group or a cyclopentyl or cycloheptyl group and/or R 2 is a fluorine, chlorine or bromine atom and/or R 3 is a ...

PROCEDURE FOR THE PRODUCTION OF RACEMI PHENYLALKYLAMINEN

PROCEDURE FOR THE PRODUCTION OF METHYLKETONEN.

FLUORENYL AZOLYLMETHYL CARBINOLE ONE, PROCEDURE FOR ITS PRODUCTION, DRUG, THESE CONNECTIONS CONTAINING AND PROCEEDING TO THE PRODUCTION OF THESE DRUGS.

VERFAHREN ZUR HERSTELLUNG NEUER ARALIPHATISCHER KETONE

PROCEDURE FOR THE PRODUCTION OF NEW OF ARALIPHATIC KETONE

Use of trifluoroacetyl alkyl-substituted phenyl derivatives, phenol derivatives and benzoyl derivatives in the treatment and/or prophylaxis of obesity and accompanying diseases and/or secondary diseases

Chalcone and its analogs as agents for the inhibition of angiogenesis and related disease states

PROCESS FOR RECOVERING PHENYLALKYLAMINES

The invention provides a process for preparing a mixture of the optical isomers of a phenylalkylamine derivative of formula(I) wherein Z is a hydrogen or chlorine atom or a trifluoromethyl, trifluoromethoxy or trifluoromethylthio radical, and R1 is a hydrogen atom or a straight or branched alkyl radical of 1 to 5 carbon atoms, or an acid addition salt thereof, by oxidising an isomer of the phenylalkylamine to the 1phenylalkyl-2-propanone which is then condensed under reductive conditions with an amine of formula HNR1R2. These compounds exhibit anorexigenic activity.

Preparation method of trifluoromethyl ketone

The invention provides a preparation method of trifluoromethyl ketone. The preparation method of the trifluoromethyl ketone comprises the following steps: (1) after being mixed, magnesium metal, solvent, halide and sodium trifluoroacetate are reacted for 0.5-2.5 hours at the temperature of 30-65 DEG C, and then are reacted for 1-3 hours at the rising temperature of 30-70 DEG C, the molar ratio of the halide and the magnesium metal is 1-1.2:1, the molar ratio of the solvent and the magnesium metal is 2-8:1, the molar ratio of the magnesium metal and the sodium trifluoroacetate is 1-1.5:1, and after the reaction finishes, obtained reaction liquid is cooled; (2) the reaction liquid is added to 2-4 mol/L of mineral acid and is acidized, an organic layer is collected, the organic layer is rectified and purified, and then the trifluoromethyl ketone is obtained. The trifluoromethyl ketone has the advantages of being low in raw material cost, low in production cost, easily purified and low in production ...

METHOD OF PREPARATION OF DERIVED FROM BIPHENYL

A-HALOGENOMETHYLPHENYLALANINES AND THEIR DERIVATIVES, USEFUL IN PARTICULAR TO TREAT THE PARKINSON'S DISEASE OR A STATE OF PSYCHOSIS, AND THEIR METHOD OF PREPARATION

5- ((3, 3, 3-TRIFLÚor-2-hidrÓXI-1-ARILPROPIL) AMINO) - 1H-QUIN OLIN-2-ONAS, a PROCESS FOR ITS PRODUCTION AND USE OF the SAME ones AS AGENTS ANTI-INFLAMATÓRIOS

HYDRAZONE DERIVATES AND INTERMEDIARY COMPOUNDS USED FOR THEIR PREPARATION

Alkylamino- and alkylamino alkyl diarylketones and pharmaceutical compositions thereof

This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula см. иллюстрацию в PDF-документе where Ar is aryl of the formula см. иллюстрацию в PDF-документе where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF3, NO2 and u is an integer of 1 to 3; X and Y are independently CH2 --, --CF2 -- or --CHF--; Z and W are independently --CH2 --, --O--, --CHOH--, or --CHF--; m, n, p, q and t are integers which are independently 0 or 1, R1 is H or loweralkyl; R2 and R3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.

Process for the preparation of 4,4-dimethyl-1-(p-chlorophenyl)pentan-3-one

... 4,4-Dimethyl-1-(p-chlorophenyl)pentan-3-one can be prepared by condensation of pinacolone and p-chlorobenzaldehyde in an alcohol as solvent in the presence of an inorganic base and by subsequent hydrogenation, in which the reaction mixture obtained in the condensation is hydrogenated directly without isolation of the intermediate 4,4-dimethyl-1-(p-chlorophenyl)-1-penten-3-one after the addition of a hydrogenation catalyst at elevated temperature and superatmospheric pressure to give 4,4-dimethyl-1-(p-chlorophenyl)pentan-3-one, after the hydrogenation catalyst has been separated off from the liquid hydrogenation mixture, the alcohol is largely distilled off, and the water content of the bottom product of the distillation is adjusted in such a manner that it separates into an aqueous and an organic phase, and the 4,4-dimethyl-1-(p-chlorophenyl)pentan-3-one is recovered from the organic phase.

Directed Beta-C(sp3)–H Iodination and Arylation of Ketones

This invention discloses the first example of palladium(II)-catalyzed β-C(sp)-H iodination or arylation of a wide range of ketones by using a commercially available aminooxyacetic acid auxiliary. This L, X-type directing group overcomes the limitation of the transient directing group approach for -βC(sp)-H functionalization of ketones. Practical advantages of this method include simple installation of the auxiliary without chromatography, exceptional tolerance of a-functional groups, double bonds and triple bonds and rapid access to diverse sterically hindered quaternary centers. 1. A method of β-C(sp)-H iodination of a ketone having a β-hydrogen substituent , comprising:contacting the ketone and an aminooxyacetic acid in pyridine solvent to provide the corresponding oxime;then,contacting the oxime with iodine in the presence of a palladium(II) salt and phenyliodoniumacetate, in an aprotic solvent; then,{'sup': '3', 'hydrolyzing the oxime group under acidic conditions to provide the product β-C(sp)-iodoketone.'}2. The method of wherein the aminooxyacetic acid is aminooxyacetic acid or 2 claim 1 ,2-dimethylaminooxyacetic acid.3. The method of wherein the palladium(II) salt is palladium(II) acetate or palladium(II)trifluoroacetate.4. The method of wherein the aprotic solvent is dioxane or 1 claim 1 ,1 claim 1 ,1 claim 1 ,3 claim 1 ,3 claim 1 ,3-hexafluoroisopropanol.5. The method of wherein the oxime group is hydrolyzed in a solution of concentrated hydrochloric acid in dioxane.6. A method of β-C(sp)-H arylation of a ketone having a β-hydrogen substituent claim 1 , comprising:contacting the ketone and an aminooxyacetic acid in pyridine solvent to provide the corresponding oxime;then,contacting the oxime with an aryl iodide and silver trifluoroacetate in the presence of a palladium(II) salt, in an aprotic solvent; then,{'sup': '3', 'hydrolyzing the oxime group under acidic conditions to provide the product β-C(sp)-arylketone.'}7. The method of wherein the ...

Process for manufacturing 1-(3-trifluoromethyl) phenyl-propan-2-one intermediate in the synthesis of the fenfluramine

Process for manufacturing 1-(3-trifluoromethyl)phenyl-propan-2-one intermediate in the synthesis of the anorexic drug fenfluramine. The process consists in reacting the diazonium salt of the 3-trifluoromethylaniline with isopropenyl acetate in a polar solvent in presence of catalytic amounts of a cuprous or cupric salt or of a mixture thereof and, optionally, of a base and inpurifying the raw product through bisulfite complex or distillation under vacuum.

Processo per la produzione di 1 - (3-trifluorometil) fenil-propan- 2-one intermedio nella sintesi della fenfluramina

PROCESSES FOR THE HYDROGENATION OF α,β-UNSATURATED KETONES

The catalytic hydrogenation of α,β-unsaturated ketones R1-CH=CH-CO-R2 in which R1 and R2 independently of one another represent straight-chain or branched C1-C12-alkyl or C2-C12-hydroxyalkyl, straight-chain or branched C2-C12-alkenyl, C3-C8-cycloalkyl, C3-C8-cycloalkenyl, C7C14-aralkyl or C6-C12-aryl, where at least one of R1 and R2 is monosubstituted to trisubstituted by halogen, to give the respective saturated ketones R11-CH2-CH2-CO-R12 in which R11 and R12 assume the meaning of R1 and R2 with the exception that alkenyl and cycloalkenyl are hydrogenated to the respective alkyl or cycloalkyl, wherein the hydrogenation process comprises combining the α,β-unsaturated ketones and a reaction medium comprising water or alcohol in amounts such that the wt% of the α,β-unsaturated ketones based on the total weight of the α,β-unsaturated ketones and the reaction medium is at least about 60 wt%, and the hydrogenation is carried out in the presence of at least (i) an organic amine, (ii) a Ni-containing catalyst, and (iii) an organic sulphur compound.

PROCESSES FOR THE HYDROGENATION OF α,β-UNSATURATED KETONES

The catalytic hydrogenation of α,β-unsaturated ketones R1-CH=CH-CO-R2 in which R1 and R2 independently of one another represent straight-chain or branched C1-C12-alkyl or C2-C12-hydroxyalkyl, straight-chain or branched C2-C12-alkenyl, C3-C8-cycloalkyl, C3-C8-cycloalkenyl, C7-C14-aralkyl or C6-C12-aryl, where at least one of R1 and R2 is monosubstituted to trisubstituted by halogen, to give the respective saturated ketones R11-CH2-CH2-CO-R12 in which R11 and R12 assume the meaning of R1 and R2 with the exception that alkenyl and cycloalkenyl are hydrogenated to the respective alkyl or cycloalkyl, wherein the hydrogenation process comprises combining the α,β-υnsaturated ketones and a reaction medium comprising a C4-C10 alcohol and water in about a 1:2 to about a 2:1 mass ratio, and the hydrogenation is earned out in the presence of (i) basic substance comprising organic amine, (ii) Ni-containing catalyst, and (iii) organic sulphur compound.

PROCESSES FOR THE HYDROGENATION OFα,β- UNSATURATED KETONES

The catalytic hydrogenation of α.β-unsaturated Ketones R1 -CH=CH-CO-R2 in which R1 and R2 Independently of one another represent straight-chain or branched C1-C12-alkyl or C2-C12-hydroxyalkyl; straight-chain or branched C2-C12-alkenyl, C3-C8-cyc[oatkyi, C3-C8-cycloalkenyl, C7-C14- aralkyl or C6-C12-aryl, where at least one of R1 and R2 is rnonosubstituted to trisubstituted by halogen, to give the respective saturated ketones R11-CH2-CH2-COR12 in which R11 and R12 assume the meaning of R1 and R2 with the exception that alkenyl and cycloalkenyl are hydrogenated to the respective alkyl or cycloalkyl, wherein the hydrogenation process comprises combining the α.β-unsaturated ketones and alcohol; the hydrogenation is carried out in the presence of (i) basic substance, (ii) Ni-containsng catalyst, and (iii) organic sulphur compound to produce product comprising the saturated ketones, the Ni-containing catalyst, and the alcohol and/or water, and the process further comprises filtering at least a portion of the Ni-containing catalyst from the product to produce filtered product; adding basic substance to the filtered product to produce an end product comprising the saturated ketones, alcohol and/or water, an inorganic chloride, and an amine; distilling at least a portion of the alcohol and at least a portion of tlie water from the end product; and filtering at least a portion of the inorganic chloride from the end product

Process for the preparation of strobilurin intermediates

The present invention relates to a novel improved process and intermediates for the process of preparing the oxime intermediates of formula (II) wherein R 1 is hydrogen, fluoro or chloro, and R 2 is methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, cyano, fluoro, chloro or bromo. The novel process comprises diazotizing an aniline of formula (VI) reacting the resulting diazonium salt with isopropenylacetate of formula (X) and reacting the resulting ketone of formula (XI) with an organic nitrite in the presence of hydrogene chloride, and methylating the resulting ketooxime of formula (VIII) with a methylating agent and reacting the resulting O-methyl ketooxime of formula (IX) with hydroxylamine. The compounds of formula (II) are intermediates for highly active fungicides from the class of the atrobilurins.

Process for the preparation of strobilurin intermediates

The present invention relates to a novel improved process and intermediates for the process of preparing the oxime intermediates of formula (II) wherein R 1 is hydrogen, fluoro or chloro, and R 2 is methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, cyano, fluoro, chloro or bromo. The novel process comprises diazotizing an aniline of formula (VI) reacting the resulting diazonium salt with isopropenylacetate of formula (X) and reacting the resulting ketone of formula (XI) with an organic nitrite in the presence of hydrogene chloride, and methylating the resulting ketooxime of formula (VIII) with a methylating agent and reacting the resulting O-methyl ketooxime of formula (IX) with hydroxylamine. The compounds of formula (II) are intermediates for highly active fungicides from the class of the strobilurins.

一种马来酸氯苯那敏杂质及其制备方法与应用

本发明涉及医药技术领域，更具体而言，涉及一种马来酸氯苯那敏杂质及其制备方法与应用。具体步骤如下：将4‑氯‑苯乙腈和氨基钠溶解于有机溶剂中，滴加少量水，反应结束后加水淬灭，水相用有机溶剂萃取，用饱和氯化铵水溶液洗涤，用有机相干燥，抽滤，浓缩得棕色液体；加入浓盐酸进行酸化反应，加热至反应结束降温，然后用氢氧化钠溶液调pH值，有机溶剂萃取，用有机相干燥，抽滤，浓缩，得到残渣为粗品；将粗品以柱层析方式纯化后，再用重结晶方法制得最终结构式2精品。本发明是在制备马来酸氯苯那敏过程中首次发现的一种新杂质，将其作为马来酸氯苯那敏原料药工艺杂质标准品或对照品，能够帮助提高马来酸氯苯那敏原料药质量控制体系。

一种西他列汀关键中间体杂质及其制备方法和应用

本发明提供了一种西他列汀关键中间体杂质及其制备方法和应用，属于药物化学技术领域。本发明提供的具有式I所示结构的化合物为合成西他列汀的关键中间体乙酰麦氏酸衍生物5‑(1‑羟基‑2‑(2,4,5‑三氟苯基)亚乙基)‑2,2‑二甲基‑1,3‑二氧杂环‑4,6‑二酮)(II)在生产过程中产生的杂质的成分，可作为对照品应用于西他列汀生产工艺中关键中间体的杂质分析，以促进关键中间体的质量控制，进而有效控制西他列汀药品的质量。本发明提供了西他列汀关键中间体杂质的制备方法，通过热解建立了西他列汀关键中间体的杂质对照品的合成方法，是研究西他列汀的杂质组成和质量控制的基础，且该方法可操作性强、方法简单。