СПОСОБ ПОЛУЧЕНИЯ 2-ЦИАНПИРАЗИНА

Изобретение относится к химической технологии, конкретно - к способу получения 2-цианпиразина, который находит широкое применение в качестве противотуберкулезного препарата. Задачей изобретения является разработка технологии получения 2-цианпиразина реакцией окислительного аммонолиза 2-метилпиразина с высоким выходом при более низкой температуре с использованием катализатора, сохраняющего высокую активность при продолжительной эксплуатации и после регенерации. Сущность изобретения: 2-метилпиразин с аммиачно-воздушной смесью пропускают через катализатор, содержащий оксида ванадия 3 - 9%, оксида хрома 2 - 7%, оксида сурьмы 1 - 3% и оксида алюминия до 100%, при 280-300oC и мольном соотношении 2-метилпиразин: аммиак: кислород 1:25 - 50: 60 - 80, при этом время контакта реакционной смеси с катализатором 0,8-1,1 с. Предлагаемый способ позволяет в более мягких условиях получать 2-цианпиразин с выходом 88 - 91% при конверсии 2-метилпиразина 98 - 99% и селективности по 2-метилпиразину 90 - 92%.

Фунгицидоинсектицидное средство

Способ получения ациламинопроизводных гетероциклических соединений

2-SUBSTITUIERTE 5-TRIFLUORMETHYL1,3,4-THIADIAZOLE, VERFAHREN ZU IHRER HERSTELLUNG SOWIE IHRE VERWENDUNG ALS FUNGIZIDE UND INSEKTIZIDE

UREA DERIVATIVES PROCESSES FOR THEIR PREPARATION AND COMPO SITIONS INCORPORATING THEM

... 1414213 Cyclic N-phenyl-urea derivatives ROUSSEL UCLAF 6 Aug 1973 [4 Aug 1972] 37189/73 Heading C2C The invention comprises an N-phenyl-urea derivative of the general Formula (I) wherein: A represents a straight- or branchedchain alkylene group containing from 2 to 6 carbon atoms; X, which may be at any available position in the benzene ring, represents a hydrogen or halogen atom, a trifluoromethyl radical, a nitro group, an acyl radical containing from 1 to 6 carbon atoms, an alkyl or alkoxy radical each containing from 1 to 6 carbon atoms, or an unsubstituted or halo-substituted alkenyloxy radical containing from 2 to 6 carbon atoms; Y, which may be at any available position in the benzene ring, represents a hydrogen or halogen atom, or an alkyl or alkoxy radical each containing from 1 to 6 carbon atoms; and R represents an alkoxy radical containing from 1 to 4 carbon atoms, an alkoxycarbonyl radical containing from 1 to 6 carbon atoms, or a chloroacetyl group. Compounds of general Formula ...

ACYLATION OF NITROGEN-CONTAINING PRODUCTS

... 1282887 Polyolefin derivatives LUBRIZOL CORP 16 June 1969 [3 July 1968] 30409/69 Heading C3P [Also in Divisions C4-C5] Polyolefin derivatives suitable as dispersants for lubricating and fuel oils may be prepared by reacting (I) polyolefin substituted mono- or polycarboxylic acylating agents with (II) not more than one mole per equivalent of I of where R is an organic radical of valence n + 1 or, where n is 1, may be a direct linkage, and n is 1 to 3; X1 and X11 are independently O= or R 1 N=; when X1 is O = then Y is or where m is 0 or 1 to 8; when X1 is R 1 N= then R 1 is -(R11-NR1)m-R11-NR1R1 and Y is -NR1-(R11-NR1) m -R11-NR1R1 or R 1 and Y together form where q is 0 or 1 to 8; when X11 is O = then Z is O-M+, halo, alkoxy or Y as defined when X1 is O = and M+ is the cation of an amine; when X11 R 1 N = then ...

Quaternary ammonium salts of antistatic agents or softening agents containing fatty acid radicals process for the production and use thereof

The present invention relates to water-soluble quaternary ammonium salts of organic compounds having antistatic or softening properties. These ammonium salts contain at least one fatty acid radical and are quaternized with a dialkyl ester of an alkylphosphonic acid. They are used for finishing organic fibrous material, especially textiles and paper.

New 2 (nitromethylene) - 1,3-diazacycloalcanes, insecticidal compositions the container and their use to fight against undesirable insects.

VERFAHREN ZUR HERSTELLUNG NEUER PYRAZOL-TRIAZOL -ODER TETRAZOLDERIVATE

FUNGICIDE AND INSECTICIDE MEANS

PYRROLIDIN AND THIAZOLIDINDERIVATE, PROCEDURES FOR YOUR PRODUCTION AND THESE CONTAINING DRUGS.

PROCEDURE FOR THE PRODUCTION OF CYCLI N, N'DIMETHYLHARNSTOFFEN.

Procedure for the production of new Phenacetylguanidine and their acid addition salts

Procedure for the production of new Phenacetylguanidine and their acid addition salts

FUNGICIDE AND INSECTICIDE MEANS

Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors

Pyrrolidine and thiazolidine derivatives, preparation thereof and drugs containing same

A 1-PYRIDYLIMIDAZOLE DERIVATIVE AND ITS PRODUCTION AND USE

2-SUBSTITUTED 5-TRIFLUOROMETHYL-1,3,4-THIADIAZOLES AND THEIR USE AS FUNGICIDES AND INSECTICIDES

Guanidine derivs as antihypertensive agents

Guanidine derivs. as antihypertensive agents Cpds. are (2-R1-6-R2-phenyl).ClH2CON=C(NR3R4)-(NR5R6) (where R1 is H, Cl or Me; R2 is Cl or Me; R3, R4, R5, R6 are the same or different and are H, alkyl, hydroxyalkyl or alkoxyalkyl of up to 6C, at least one being other than H, or R4 and R5 together are -(CH2)2- or -(CH2)3 and R3 and R6 are each H) and the salts thereof.

Guanidine derivs as antihypertensive agents

Guanidine derivs. as antihypertensive agents Cpds. are (2-R1-6-R2-phenyl).ClH2CON=C(NR3R4)-(NR5R6) (where R1 is H, Cl or Me; R2 is Cl or Me; R3, R4, R5, R6 are the same or different and are H, alkyl, hydroxyalkyl or alkoxyalkyl of up to 6C, at least one being other than H, or R4 and R5 together are -(CH2)2- or -(CH2)3 and R3 and R6 are each H) and the salts thereof.

Verfahren zur Herstellung von Acylguanidinen

PROCEDE DE PREPARATION DE COMPOSESDERIVES ACYLAMINO DE HETEROCYCLIQUES.

[...] DE [...] DE [...] PHENYL- [...][...].

PROCEDE DE PREPARATION DE COMPOSESDERIVES ACYLAMINO DE HETEROCYCLIQUES.

Pesticide containing 2-(nitromethylene)-1,3-diazacycloalkanes

QUATERNAERE AMMONIUM SALTS OF FATTY ACID REMAINDER OF EXHIBITING ANTISTATIKA OR SOFT GRASP MEANS, THEIR PRODUCTION AND USE.

4-DIHYDRO-2H,6H-PYRIMIDO[2,1-B][1,3,5]THIADIAZIN-7-CARBONITRILE

4-DIHYDRO-2H,6H-PYRIMIDO[2,1-B][1,3,5]THIADIAZIN-7-CARBONITRILE

8-,4-DIHYDRO-2H,6H-PYRIMIDO[2,1-B][1,3,5]THIADIAZIN-7-CARBONITRILE

PROCESS FOR THE PREPARATION OF ALKYLIMIDAZOLIDONE (METH-) ACRYLATE COPOLYMERS.

SELS D'AMMONIUM QUATERNAIRE DE PRODUITS ANTISTATIQUES OU D'AGENTS ADOUCISSEURS DU TOUCHER PRESENTANT DES RESTES D'ACIDE GRAS, LEUR PROCEDE DE PREPARATION ET LEUR UTILISATION

Sels d'ammonium quaternaire de produits antistatiques ou d'agents adoucisseurs du toucher présentant des restes d'acide gras, leur procédé de préparation et leur utilisation. Ces sels ayant la formule : ...

Substd benzamido alkylamidines and cyclic amidines - useful as analgesic agents, obtd. by N-acylating substd. amino alkyl cyanide

TRIARYL COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R3a, R4, R6, R7, R8, A, Z, X1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

SUBSTITUTED DIHYDRO-BENZIMIDAZOLE COMPOUNDS AS ROR GAMMA MODULATORS

The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as modulator of retinoid-related orphan receptor gamma t (RORyt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated disease, disorder, syndrome or condition such as pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, neurodegenerative diseases or cancer.

Bisguanidines and fungicides containing them

The present invention relates to bisguanidine derivatives of the formula I см. иллюстрацию в PDF-документе where R1 and R2 are each, independently of one another, hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5-12 carbon atoms in the ring and may be substituted, or benzyl which may be substituted, with the proviso that only one of R1 and R2 can be hydrogen; or R1 and R2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted; X is CH2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted, n is 5 to 8, and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.

ПРОИЗВОДНЫЕ 1-ПИРИДИЛИМИДАЗОЛА И ИНСЕКТИЦИДНАЯ КОМПОЗИЦИЯ

Использование: в сельском хозяйстве, в частности в качестве инсектицидных средств. Сущность изобретения: продукт - производные 1-пиридилимидазола ф-лы 1, где R1 - H, C1-C3 -алкил, R2 - C1-C4 - галоидалкил; R3 - галоген или трифторметил. R4 - C1 -C3 - галоидалкил. Инсектицидная композиция содержит указанные активные ингредиенты в количестве 0,1 - 95% и остальное целевые добавки. 2 с.п. ф-лы, 8 табл. Структуры ф-лы 1: ...

(Е)-(6-(2-гидроксифенил)-2-иминио-4,7,8-триоксо-1,3-дифенил-1,3,6-триазаспиро[4.4]нонан-9-илиден)(4-метоксифенил)метаноат, обладающий противомикробной активностью, и способ его получения

Изобретение относится к области органической химии, а именно к новому индивидуальному соединению (Е)-(6-(2-гидроксифенил)-2-иминио-4,7,8-триоксо-1,3-дифенил-1,3,6-триазаспиро [4.4] нонан-9-илиден) (4-метоксифенил)метаноату и к способу его получения. Технический результат: получение индивидуального соединения (Е)-(6-(2-гидроксифенил)-2-иминио-4,7,8-триоксо-1,3-дифенил-1,3,6-триазаспиро [4.4] нонан-9-илиден) (4-метоксифенил)метаноата, обладающего противомикробной активностью, и разработка простого способа его получения, который может быть использован в качестве исходного продукта для синтеза новых гетероциклических систем и в фармакологии. 2 н.п. ф-лы, 1 табл., 2 пр.

Способ получения сульфонильных соединений

SUBSTITUIERTE PHENYLAMIDINE UND DIESE ENTHALTENDE ARZNEIMITTEL

Verfahren zur Herstellung von Alkylimidazolidonmethacrylaten

Polymerisierbare cyclische Harnstoffderivate und Polymere mit angehängter Harnstoffgruppe.

SULPHONYL COMPOUNDS

... 1358774 Novel sulphonyl derivatives CASSELLA FARBWERKE MAINKUR AG 5 June 1972 [5 June 1971] 26140/72 Heading C2C [Also in Division C3] The invention comprises novel compounds having the formula R-SO 2 -X wherein X is a moiety of formula and wherein R and R5 are phenyl, naphthyl, benzyl, phenylethyl, thienyl, pyrrolyl, carbazolyl, pyridyl, phenothiazinyl, C 4 -C 8 cycloalkyl, C 1 -C 8 alkyl any of which may be substituted by an alkyl, alkoxy, alkanoyl, C 1 -C 4 alkanoyloxy, alkanoylamino or dialkylamino, -OH, -CN, -Cl, -F, -Br, -NO 2 , -CF 3 , or -CO 2 -; R 1 and R 4 are H, -CO 2 - or a group as defined for R; R2 is phenyl, naphthyl, bedzyl, phenylethyl, C 4 -C 8 cycloalkyl or C 1 -C 8 alkyl any of which may be substituted by alkyl, alkoxy, C 1 -C 4 alkanoyl, alkanoyloxy or dialkylamino group, OH, CN, Cl, F, Br, NO 2 , CF 3 or -CO 2 -; R3 is H or a group as defined for R2; Y is C 1 -C 8 alkylene, C 4 -C 8 cycloalkylene or phenylene, Y1 is a direct ...

VERFAHREN ZUR HERSTELLUNG NEUER HARNSTOFF- UND AMIDO-VERBINDUNGEN

PROCEDURE FOR THE PRODUCTION OF NEW UREA AND AMIDO CONNECTIONS

PROCEDURE FOR THE PRODUCTION OF ALKYLIMIDAZOLIDONE (METH) ACRYLATE.

PROCEDURE FOR THE PRODUCTION OF NEW SULPHONYL CONNECTIONS

PROCEDURE FOR THE PRODUCTION OF NEW PYRAZOL TRIAZOL - OR TETRAZOLDERIVATE

NOVEL 2-%NITROMETHYLENE<-1,3-DIAZACYCLOALKANES

1,3,4-THIADIAZOLES

2- (NITROMETHYLENE)-1,3-DIAZACYCLOALKANE INSECT CONTROL AGENTS

The present invention relates to novel insecticides of the general formula wherein n is 2, 3 or 4; R1 is alkyl, haloalkyl, alkoxyalkyl, epoxyalkyl, alkylthioalkyl, alkanoyloxyalkyl, alkenyl, haloalkenyl, alkynyl, hydroxy, amino, mono- or dialkylamino or halogen; R2 represents hydrogen, halogen, nitro or alkyl; R3 represents alkyl and m is 0 or 1. Especially compounds wherein n is 2 or 3, R1 represents methyl, 2-propenyl, 3-chloro-2-propenyl or 2-propynyl and R2 is hydrogen, m being 0 have demonstrated high activities.

A 1-PYRIDYLIMIDAZOLE DERIVATIVE AND ITS PRODUCTION AND USE

A novel pyridylimidazole derivative having the formula; wherein R1 is a hydrogen atom, a C1-C3 alkyl group, a C1-C3 alkylthio group or a C2-C3 alkoxyalkyl group; R2 is a hydrogen atom or a C2-C4 haloalkyl group; R3 is a halogen atom, a nitro group or a trifluoromethy group; R4 is a C1-C3 haloalkyl group or a C1-C3 haloalkoxy group, a process for producing the same and insecticides containing the same as an active ingredient, are disclosed.

A 1-PHENYLIMIDAZOLE DERIVATIVE AND ITS PRODUCTION AND USE

A novel 1-phenylimidazole derivative having the formula: wherein R is a hydrogen atom or a methyl group; X is a fluorine atom, a chlorine atom or a nitro group; Y is a fluorine atom or a chlorine atom; Z is a hydrogen atom, a fluorine atom, a chlorine atom or a bromine atom, a process for producing the same and insecticides containing the same as an active ingredient, are disclosed.

FUNGICIDAL COMPOSITIONS, FUNGICIDAL COMPOUNDS, THEIR PRODUCTION AND USE

... 2066164 9105473 PCTABS00005 Agricultural fungicidal compositions comprising compounds of formula (I-A), (I-B) or (I-C), wherein R1 and R7 are each independently hydrogen or C1-C3 alkyl, R2 is hydrogen or C1-C6 alkyl, R3 and R4 independently, and each R5 independently are hydrogen or C1-C4 alkyl, R6 is a cyclohexyl group or a monocyclic or bicyclic aromatic group, substituted with from 1 to 5 groups of the formula R8, wherein R8 is halogen, a C1-C10 alkyl group, a C1-C10 alkoxy group, a tri-C1-C4-alkylsilyl group, or a phenoxy, phenyl, phenyl-C1-C2-alkylene, or phenyl-C2-alkenylene group, each optionally substituted on the phenyl or phenoxy group with one or more of halogen atoms, C1-C6 alkyl or C1-C6 alkyl or C1-C6 alkoxy groups, trihalomethyl groups, phenyl groups or phenoxy groups. p is 0, 1 or 2, Y is a group of the formula -(CR9R9)n-, wherein n is 2, 3, or 4, each R9 independently is hydrogen or C1-C4 alkyl and X is a suitable counter-ion, together with an agriculturally acceptable ...

4-DIHYDRO-2H,6H-PYRIMIDO[2,1-B][1,3,5]THIADIAZIN-7-CARBONITRILE

Piperidine - substituted inhibitors of Mnk and related methods

3-(4-ETHOXYPHENYL)-8-(4-METHYLPHENYL)-6-OXO-3,4-DIHYDRO-2H,6H-PYRIMIDO[2,1-B][1,3,5] THIADIAZIN-7-CARBONITRILE

НЕТОКСИЧНОЕ ПРОИЗВОДНОЕ β-(БЕНЗИМИДАЗОЛ-1-ИЛ) ПРОПИОАМИДОКСИМА, АКТИВНОЕ ПРИ ЛЕЧЕНИИ ЭКСПЕРИМЕНТАЛЬНОГО ТУБЕРКУЛЕЗА

Изобретение относится к медицине, а именно к фармакологии. Производное β-(бензимидазол-1-ил) пропиоамидоксима предлагается использовать в качестве средства при терапии туберкулеза, вызванного чувствительными штаммами М. tuberculosis H37Rv. Преимуществом является снижение острой подкожной токсичности предлагаемого соединения в 3,73 раза по сравнению с рифампицином при сравнимой in vivo противотуберкулезной активности на чувствительных штаммах М. tuberculosis H37Rv.

2, 3-diaryl thiazolinone compound and usage thereof in preparation of medicine for treating tumour

The invention discloses a 2, 3-diaryl thiazolinone compound shown in a structural formula (I), or hydrate or pharmaceutically acceptable salt of the 2, 3-diaryl thiazolinone compound, a pharmaceutical composition containing the 2, 3-diaryl thiazolinone compound, and application of the 2, 3-diaryl thiazolinone compound in preparation of a medicine for treating various cancers and related diseases caused by tumor metastasis.

QUATERNARY AMMONIUM SALTS OF ANTI-STATIC PRODUCTS OR AGENTS SOFTENERS OF the TOUCH PRESENTING OF the REMAINDERS Of Fatty-acid, THEIR METHOD OF PREPARATION AND THEIR USE

COMPOSES SULFONYLIQUES

SELECTIVE BTK IRREVERSIBLE INHIBITORS

The invention provides a series of conformationally stable and selective, irreversible kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds. The compounds herein are atropisomers having increased kinase selectivity and are for use in treating conditions that benefit from selective BTK kinase inhibition.

A MOLECULAR GLUE REGULATING CDK12-DDB1 INTERACTION TO TRIGGER CYCLIN K DEGRADATION

Provided is a new kind of molecular glues for triggering polyubiquitination and degradation of CCNK (cyclin K). Specifically, a new kind of molecular glues for creating a modified CDK12 protein so as to bind DDB1 of DDB1-CUL4-RBX1. The molecular glues convert CDK12 into a substrate-specific receptor to trigger the polyubiquitination and subsequent degradation of CDK12's partner protein CCNK.

COMPOUNDS AND THERAPEUTIC USES THEREOF

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, diseases associated with over production of IL12/IL23, lysosomal storage disorders, filovirus infections, ischemia, and other complications associated with these diseases and disorders.

Non-metal tanning process

Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or belt with a tanning agent (A) of at least a mixture of compounds of formula (I) and formula (II), wherein Hal signifies fluorine or chlorine, R1 signifies hydrogen, C1-8-alkyl or an alkyleneoxy radical of formula (III), —(—C2-3 alkylene-O—)q—H (III); R2 signifies a) phenyl, mono- or di-substituted with SO3M or COOM and optionally substituted also with hydroxyl, C1-4-alkyl C1-4-alkoxy; b) naphthyl, mono- or di- or tri-substituted with SO3M and optionally substituted also with hydroxyl; c) C1-8-alkylene, substituted with (SO3M) or (COOM); d) aradical of formula (IV), —(—C2-3 alkylene-O—)p—Y (IV) or e) a radical of formula (IVa) —(C2-3 alkylene-O)p—C2-3 alkylene-SO2CH2CH2O—Y (IVa), M signifies 1 or 2, p signifies 0 or 1, Y signifies hydrogen or —SO3M, q signifies 1 to 10, M signifies hydrogen, an alkali metal cation or an ammonium cation being aprotonated tertiary amine or a ...

Cyclopropylamines as pharmaceuticals

The present invention relates to cyclopropylmethyl amines substituted by a heterocyclic radical.

PROCESS FOR THE PREPARATION OF ALKYLIMIDAZOLIDONE (METH) ACRYLATE

At least one (meth)acrylate is reacted with a heterocyclic alcohol (III) in the presence of at least one catalyst chosen from dialkyltin oxides and dialkyltin dialkoxides. Alkylimidazolidone acrylates and methacrylates are known for the part they play in the constitution of polymers which can be used as coatings and adhesives and for the treatment of paper and textiles, and for their use as agents for the treatment of leather and in the production of emulsion paints. (I) (II) (III) R1=H, CH3 ; A, B=straight or branched chain alkylene group containing from 2 to 5 carbon atoms.

FUNGICIDAL COMPOSITIONS, FUNGICIDAL COMPOUNDS, THEIR PRODUCTION AND USE

Agricultural fungicidal compositions comprising compounds of formula (I-A), (I-B) or (I-C), wherein R1 and R7 are each independently hydrogen or C1-C3 alkyl, R2 is hydrogen or C1-C6 alkyl, R3 and R4 independently, and each R5 independently are hydrogen or C1-C4 alkyl, R6 is a cyclohexyl group or a monocyclic or bicyclic aromatic group, substituted with from 1 to 5 groups of the formula R8, wherein R8 is halogen, a C1-C10 alkyl group, a C1-C10 alkoxy group, a tri-C1-C4-alkylsilyl group, or a phenoxy, phenyl, phenyl-C1-C2-alkylene, or phenyl-C2-alkenylene group, each optionally substituted on the phenyl or phenoxy group with one or more of halogen atoms, C1-C6 alkyl or C1-C6 alkyl or C1-C6 alkoxy groups, trihalomethyl groups, phenyl groups or phenoxy groups. p is 0, 1 or 2, Y is a group of the formula -(CR9R9)n-, wherein n is 2, 3, or 4, each R9 independently is hydrogen or C1-C4 alkyl and X is a suitable counter-ion, together with an agriculturally acceptable carrier or diluent, and novel ...

Способ получения циклопропиламинов или их солей

Способ получения ациламинозамещенных гетероциклов

Hypoglycaemic (2)-substd. (1,3)-diaza-heterocyclic cpds. - e.g. (2)-benzhydrylimino-imidalodine prepd. e.g. by reacting (2)-mercapto-imidazolines with amines

New 2-substd. 1-3-diaza heterocyclic cpds. are of formula (I) and their salts. In the formula R1 is H, halogen, lower alkyl or lower alkoxy; R2 is H, lower alkoxycarbonyl, aliphatic acyl, or aromatic acyl the aromatic ring of which may be substd. by halogen, lower alkyl, lower alkoxy, acyl and/or acyloxy. R3 is H, lower alkyl, lower hydroxyalkyl or aralkyl, R4 is H, lower alkyl or aryl. R6 is cyclohexyl, pyridyl, or phenyl opt. substd. by halogen, lower alkyl or lower alkoxy. A is -N=, -N(lower alkyl)- or CH2. n is 2, 3 or 4. Broken lines indicate the optional presence of a double bond. (I)have hypoglycaemic and blood platelet aggregation inhibiting activity, and are free from undesirable side-effects. Specific (I) include 2-benzhydrylimino-imidazolidine. In an example, this is prepd. by refluxing 7.3 g benzhydrylamine and 4.88 g 2-methylthio-2-imidazoline hydriodide 3 hrs. in 10 ml methanol.

VERFAHREN ZUR HERSTELLUNG VON SUBSTITUIERTEN 1,3-DIARYL-2-IMINO-IMIDAZOLIDINEN UND -2-IMINO-HEXA-HYDROPYRIMIDINEN

1,3-DIARY-2-IMINO-IMIDAZOLIDINES OR HEXAHYDROPYRIMIDES

PROCEDURE FOR THE PRODUCTION OF NEW PYRAZOL) TRIAZOL - OR TETRAZOLDERIVATE

Procedure for the production of new hetero-cyclic connections and their acid addition salts

PROCEDURE FOR THE PRODUCTION OF ALKYLIMIDAZOLIDONMETHACRYLATEN

ECTOIN AND ECTOINDERIVATE AS HUMIDITY DONORS IN KOSMETIKPRODUKTEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN CYCLOPROPYLMETHYLAMINEN UND IHREN SALZEN UND OPTISCHEN ISOMEREN

PROCEDURE FOR THE PRODUCTION OF NEW CYCLOPROPYLMETHYLAMINEN AND YOUR SALTS AND OPTICAL ISOMERS

FUNGIZIDES UND INSEKTIZIDES MITTEL

UNTIL GUANIDINE ONE AND THIS CONTAINING FUNGICIDES.

PROCEDURE FOR THE PRODUCTION OF NEW CYCLOPROPYLMETHYLAMINEN AND YOUR SALTS AND OPTICAL ISOMERS

ACYLAMINO DERIVATIVES

2-SUBSTITUTED 5-TRIFLUOROMETHYL-1,3,4-THIADIAZOLES AND THEIR USE AS FUNGICIDES AND INSECTICIDES

The application relates to certain new 2-substituted fluoromethyl-1,3,4-thiadiazoles and to their use as fungicides and insecticides. The application also relates to a process for the of the compounds, in which as an example a fluoromethyl-1,3,4-thiadiazole is reacted with a and, if required, the resultant 2-substituted 5-trifluoro-methyl-1,3,4-thiadiazole is reacted with an oxidising agent. The active compounds have a broad spectrum of action and can be employed against parasitic fungi and bacteria in the field of plant protection.

PIPERIDINE-SUBSTITUTED MNK INHIBITORS AND METHODS RELATED THERETO

The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof wherein X1, X2, R1, R2, R3 and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

GLYCOSYLATED SPHINGOID BASES AND PRODUCTION THEREOF

The present invention relates to several novel 1-O-glycosylated sphingoid bases and to a production method thereof, as well as to uses of the 1-O-glycosylated sphingoid bases. Sphingoid bases carrying a vinylogous amide-type protecting group are used herein for the production of 1-O-glycosylated sphingoid bases. These vinylogous amide compounds enable an easy and effective production of 1-O-glycosylated sphingoid bases. The sphingoid bases carrying a vinylogous amide-type protecting group have formulas l-lll below: General Formula I, General Formula II, General Formula III.

PROCEDES DE PREPARATION DE COMPOSES CYCLISES COMPORTANT UN GROUPEMENT UREE

PROCESS FOR THE PREPARATION OF ALKYL IMIDAZOLIDONE (METH)ACRYLATE

On prépare un composé (I) en faisant réagir au moins un (méth)acrylate (II) avec un alcool hétérocyclique (III), en présence d'au moins un catalyseur choisi parmi les dialkyloxydes d'étain, les dialkyldialcoxydes d'étain. Les acrylates et méthacrylates d'alkylimidazolidone sont connus pour leur rôle dans la constitution de polymères utiles comme revêtements et adhésifs, et pour le traitement du papier et des textiles, ainsi que pour leur utilisation comme agents de traitement du cuir et dans la production de peintures en émulsion. R1 = H, CH3; A, B = groupe alkylène à chaîne droite ou ramifiée ayant de 2 à 5 atomes de carbone.

PYRROLIDINE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME

... 2102697 9301167 PCTABS00161 Composés de formule (I) leurs sels, leur préparation et les médicaments les contenant.

SUBSTITUTED CYCLOPROPYLMETHYLAMINES PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

METHOD OF PREPARATION OF (METH) ACRYLATES Of ALKYLIMIDAZOLIDONE

On prépare un composé (I) par réaction d'au moins un (méth)acrylate (II) avec un alcool hétérocyclique (III), en présence d'un catalyseur constitué par un mélange formé (a) d'au moins un alcoolate de magnésium et (b) d'un composant choisi parmi les chélates de calcium avec les composés 1,3-dicarbonylés, les dialkyloxydes d'étain, les dialkylalcoxydes d'étain et les dialkyldiesters d'étain. (CF DESSIN DANS BOPI) R = alkyle en C1 -C4 . R**1 = H, CH3 ; A, B = chaîne hydrocarbonée droite ou ramifiée en C2 -C5 ; R**2 = alkyle en C1 -C4 .

NEWS 1,3-DIARYL-2-IMINO-IMIDAZOLIDINES AND 1,3-DIARYL-2-IMINO-HEXAHYDRO-PYRIMIDINES SUBSTITUEES, METHODS OF PREPARATION OF THESE COMPOSE AND DRUGS the CONTAINER

NEW 1.3-TO-DIARYL 2-IMINO IMIDAZOLIDINE AND 1.3 TO-DIARYL 2-IMINO-HEXAHYDRO-PYRIMIDINE [...], METHODS FOR THEIR PREPARATION AND MEDICAMENTS CONTAINING THEM

Inhibitors of cyclin-dependent kinase 7 (CDK7)

The present invention provides various compositions, including compounds of Formula (I) or (Ia), or a species thereof, and pharmaceutically acceptable salts, solvates (e.g., hydrates), stereoisomer, tautomers, and isotopic forms thereof. Also provided are methods (or uses) and kits involving the compounds or pharmaceutically acceptable formulations for treating or preventing a disease (e.g., a proliferative disease) in a subject. Administration of a compound or pharmaceutical composition described herein may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis in the subject.

CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1

This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell. 2. The compound of wherein claim 1 ,{'sup': 1a', '1b, 'sub': 1', '6', '2', '6', '2', '6', '1', '3', '1', '3', '1', '3', '2, 'Rand Rare each independently (a) hydrogen or (b) (C-C)alkyl, (C-C)alkenyl, (C-C)alkynyl or (C-C)alkoxy(C-C)alkyl, each of which are optionally substituted with up to three groups independently selected from fluorine, hydroxy, (C-C)alkoxy and HNC(═O);'}{'sub': 1', '8', '2', '8', '2', '8', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4, 'A is straight or branched (C-C)alkyl, (C-C)alkenyl or (C-C)alkynyl, each of which are optionally substituted with up to 4 groups independently selected from fluorine, cyano, oxo, R, RO—, (R)N—, ROC—, RS, RS(═O)—, RS(═O)—, RC(═O)NR—, (R)NC(═O)—, (R)NC(═O)O—, (R)NC(═O)NR—, ROC(═O)NR—, (R)NC(═NCN)NR—, (RO)P(═O)O, (RO)P(═O)NR—, ROS(═O)NR—, (R)NS(═O)O—, (R)NS(═O)NR—, RS(═O)NR—, RS(═O)NHC(═O)—, RS(═O)NHC(═O)O—, RS(═O)NHC(═O)NR—, ROS(═O)NHC(═O)—, ROS(═O)NHC(═O)O—, ROS(═O)NHC(═O)NR—, (R)NS(═O)NHC(═O)—, (R)NS(═O)NHC(═O)O—, (R)NS(═O)NHC(═O)NR—, RC(═O)NHS(═O)—, RC(═O)NHS(═O ...

Crystalline Pharmaceutical

New crystalline forms of lopinavir are disclosed. 1. A hydrated crystalline form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 7.25°±0.1° , 8.53°±0.1° , 10.46°±0.1° , 11.05°±0.1° , 11.71°±0.1° , 14.76°±0.1° , 15.30°±0.1° , 16.67°±0.1° , 17.32°±0.1° , 19.10°±0.1° , 19.57°±0.1° , 21.24°±0.1° , 21.84°±0.1° and 22.46°±0.1°.2. A higher hydrated crystalline form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 3.89°±0.1° , 6.55°±0.1° , 7.76°±0.1° , 8.55°±0.1° , 9.70°±0.1° , 10.56°±0.1° , 14.76°±0.1° , 15.57°±0.1° , 18.30°±0.1° , 18.95°±0.1° and 22.74°±0.1°.3. A higher hydrated crystalline form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 3.89°±0.1° , 6.55°±0.1° , 7.76°±0.1° , 8.55°±0.1° , 9.70°±0.1° , 10.56°±0.1° , 14.76°±0.1° , 15.06°±0.1° , 15.57°±0.1° , 16.49°±0.1° , 17.51°±0.1° , 18.30°±0.1° , 18.95°±0.1° , 21.73°±0.1° and 22.74°±0.1°.4. A solvated crystalline form of lopinavir with characteristic peaks in the solid state infrared spectrum at a position within the ranges of 1661-1673 cm , 1645-1653 cmand 1619-1629 cm.5. A desolvated crystalline form of lopinavir with at least one characteristic peak in the solid state infrared spectrum at a position within the range 1655-1662 cm.6. A desolvated crystalline form of lopinavir with characteristic peaks in the solid state infrared spectrum at a position within the ranges of 1655-1662 cmand 1636-1647 cm.7. A desolvated crystal form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 4.85°±0.1° , 6.39°±0.1° , 7.32°±0.1° , 8.81°±0.1° , 12.20°±0.1° , 12.81°±0.1° , 14.77°±0.1° , 16.45°±0.1° and 17.70°±0.1°.8. A desolvated crystal form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 4.85°±0.1° , 6.39°±0.1° , 7.32°±0.1° , 8.81°±0.1° , 12.20°±0.1° , ...

METHOD OF OBTAINING ACCORDINGLY FIXED PHENACETHILGUANIDINE

Method for producing substituted phenyl acetylguanidine

Patent FR2034557A1

Manufacturing process for cyclic urea derivatives

Process for preparing 2-thione-4, 4, 6-trimethyltetrahydropyrimidine

Improvements made to the preparation of imidazolines substituted in position 2

Patent FR1595659A

Patent FR2034557B1

Acetyl guanidine derivatives

Lopinavir prepared by one-pot method

一锅法制备洛匹那伟(I)， 其由2,6‑二甲基苯氧基乙酸、羧基活化剂、式(III)所示化合物在有机溶剂中进行缩合反应

Nucleic acid transfer agent useful for transfecting cells, especially muscle cells in vivo

Nucleic acid transfer agent comprises a cyclic amidine derivative (I). Nucleic acid transfer agent comprises a cyclic amidine derivative of formula (I). CA = cyclic amidine derivative of formula (i) or (ii): m, n = 0-3; R1 = -((CH2)p-Y)q-; p, q = 0-10; Y = CO, NH, NMe or CH2; X = NR2 or CHR2; R2 = H or R1; Z = CHR''' or NR'''; R' - R''' = H, Me or R1; Sep = a direct bond or -(NR4-(CHR3)r)t-CO- with N attached to CA; t = 0-8; r = 0-10; R3 = H, Me or -((CH2)s-NR5)u-H; u = 1-10; s = 2-8; R5 = H, CA or -((CH2)s-NR5)u-H; R4 = R3 or CA; R = NR6R7, a steroid derivative or -(NH-(CH2)x)y-Q; R6, R7 = H or optionally fluorinated 1-22C (un)saturated aliphatic group, with at least one of R6 or R7 different from hydrogen and the other containing 10-22C; x = 1-8; y = 1-10; Q = CONR6R7 or COR8; R8 = OR9 or a group of formula (iii): z = 2-8; R9 = an optionally fluorinated 8-22C (un)saturated aliphatic group or a steroid derivative; and provided that m + n = 1 or more, that R'' and R''' can not be both R1, and that R' and R''' cannot be both R1. An Independent claim is also included for: (1) a composition containing (I) and a nucleic acid; (2) a method for transferring DNA comprising contacting the nucleic acid with (I) to form a complex and contacting the cells with the complex; or for transfer of nucleic acids into cells in vivo; and (3) the preparation of nucleic acid transfer agent.

Process for the preparation of hexahydropyrimidine derivatives

2-imino derivatives of substituted imidazoles

A class of 2-imino derivatives of substituted imidazoles are prepared and are useful to regulate the natural growth or development of plants. Representative of this class of imidazoles is 1-isopropyl-2-((3-methoxypropyl)imino)-3-(3,4-dichlorophenyl)4-methyl-4 -imidazoline oxalate.

NOVEL NUCLEIC ACID TRANSFER AGENTS, COMPOSITIONS CONTAINING THEM AND USES THEREOF

A kind of organic solvent recrystallization purification butylene pitches the method and device of two ureas

本发明涉及一种利用有机溶剂重结晶提纯丁烯叉二脲的方法及装置，该方法包括溶解与热过滤、冷却重结晶、以及洗涤与干燥步骤，最终得到了提纯的丁烯叉二脲纯品。热溶解过程用到了专门设计的多滤芯双层夹套恒温过滤器，该过滤器具有相互连通的内层夹套和外层夹套，过滤器的漏斗喉部装有吸附滤芯和过滤滤芯。与现有技术相比，本发明的方法简便易行，适用于放大进行大规模生产，具有产量高，成本低，耗时短等特点，经液相色谱及质谱分析表明提纯后的丁烯叉二脲产品纯度高，品质好；还可以进行循环精制，逐步提高产品品质和附加值，具有广阔的应用前景。

Process for the preparation of substituted tetrahydropyrimidinone derivatives

Known, herbicidally active, substituted tetrahydropyrimidinone derivatives of the general formula <IMAGE> in which Ar<1> and Ar<2> are identical or different and represent optionally substituted aryl and R<1>, R<2> and R<3> represent hydrogen or lower alkyl, are obtained by a novel process by reacting N,N'-disubstituted ureas of the general formula II, <IMAGE> with 1,3-dihaloalkanes of the general formula III <IMAGE> in which Hal<1> and Hal<2> are identical or different and represent halogen, in the presence of a diluent and in the presence of a strong base and, if appropriate, in the presence of a catalyst, at temperatures between +20 DEG C and +160 DEG C.

Pyrimidinone synthesis

4-(3,4-dichlorophenyl)-2-(methylamino)-2-imidazoline

4-(3,4-DICHLOROPHENYL)-2-(METHYLAMINO)-2-IMIDAZOLINE Abstract of the Disclosure The imidazoline 4-(3,4-dichlorophenyl)-2-(methylamino)-2-imidazoline and non-toxic pharmaceutically acceptable acid addition salts thereof are useful as antihypertensive agents. Displacement of the methyl mercapto grouping from 2-methylthio-4-(3,4-dichlorophenyl)-2-imidazoline with methylamine provides the imidazoline of the present invention.

一种洛匹那韦的新晶型及其制备方法

本发明适用于药物化学领域，提供了一种洛匹那韦的新晶型及其制备方法；所述的新晶型的X射线粉末衍射图中在2θ为5.179°±0.02°、7.508°±0.02°、9.235°±0.02°、10.532°±0.02°、12.015°±0.02°、14.475°±0.02°、16.154°±0.02°、18.123°±0.02°的位置处有特征峰。新晶型样品的X‑射线衍射图具有特征性，经过红外光谱，HPLC和DSC证实洛匹那韦在晶型转变后并未发生化学结构的变化，且在热力学、化学稳定性上均有显著提高。同时本发明提供了所述新晶型的制备方法，该方法在实现上简单、高效，回收率高，适用于大批量的工业化生产。

一种1,3-二甲基丙撑脲的连续化制备方法

一种1,3‑二甲基丙撑脲的连续化制备方法，其属于有机合成领域。该方法以丙烯脲为原料，以甲醛、甲酸为甲基化试剂，在一定的温度和压力下，通过微通道反应器进行甲基化反应，经减压浓缩，得到1,3‑二甲基丙撑脲。本发明提供一种1,3‑二甲基丙撑脲的连续化制备工艺方法，整个反应体系实现智能连续化，制备方法简单，反应时间较短，产品收率达到75‑80%，提高产能。

Derives d'allantoine et d'acides amines basiques, leur procede de preparation et leur application

Les composés d'allantoine et d'acides aminés basiques selon l'invention ont une solubilité qui est de 25 à 50 fois supérieure à celle de l'allantoïne pure. Ces composés présentent presque les mêmes effets pharmacologiques que l'allantoine et les acides aminés basiques et ils sont moins toxiques. Ces composés peuvent être utilisés dans des médicaments, des cosmétiques, des crèmes et des onguents.

Verbindungen des allantoins mit basischen aminosaeuren und verfahren zu ihrer herstellung

Process for preparing (s)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2h)- pyrimidineacetic acid

Procedimento per la preparazione dell'acido (s)-tetraidro-a-(1-metiletil)-2-osso-1(2h)-piridinacetico

[UNK]

Verfahren zur herstellung von im wesentlichen ameisensäure-freien n-alkyl-n'- methylalkylenharnstoffen

[UNK]

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Derivate von 2-Amino-imidazol-2-in und Verfahren zu deren Herstellung sowie diese Derivate enthaltende Medikamente

Derives de l'amino-2 imidazoline-2, leur preparation et les medicamentsqui les contiennent

制备基本上无甲酸的n－烷基－n′－甲基亚烷基脲的方法

本发明涉及一种在甲酸存在下,通过由相应的亚烷基脲与单或多聚甲醛反应制备下式所示的基本上无甲酸的N－烷基－N’－甲基亚烷基脲的方法,式中各基团的定义如说明书所述,该方法包括:将反应所得的N－烷基－N’－甲基亚烷基脲和甲酸的混合物送至蒸馏塔的上部,不附加额外步骤进行蒸馏,并在蒸馏塔的下部排出基本上无甲酸的N－烷基－N’－甲基亚烷基脲,设定反应参数使得塔上部的压力高于塔下部的压力,塔上下两部的压力差为10～100毫巴;塔下部的温度高于塔上部的温度,塔上下两部的温度差为40℃－210℃。

Verfahren zur Herstellung von im wesentlichen Ameisensäure-freien N-Alkyl-N'-methylalkylenharnstoffen

Die Erfindung betrifft ein Verfahren zur Herstellung von im wesentlichen Ameisensäure-freien N-Alkyl-N'-methylalkylenharnstoffen der Formel mit R 1 = H oder CH 3 , R 2 = C n H 2n+1 mit n = 1-4 und x = 0 oder 1, aus den entsprechenden Alkylenharnstoffen durch Umsetzung mit monomerem oder polymerisiertem Formaldehyd in Gegenwart von Ameisensäure. Dabei wird das bei der Umsetzung erhaltene Gemisch aus N-Alkyl-N'-methylalkylenharnstoff und Ameisensäure dem oberen Bereich einer Destillationskolonne zugeführt, ohne weitere Zusätze destilliert und dem unteren Bereich der Kolonne im wesentlichen Ameisensäure-freier N-Alkyl-N'-methylalkylenharnstoff entnommen. Die Verfahrensparameter werden so eingestellt, daß der Druck im oberen Bereich der Kolonne höher ist als im unteren Bereich der Kolonne und der Differenzdruck zwischen dem oberen und dem unteren Bereich der Kolonne 10 bis 100 mbar beträgt, und daß die Temperatur im unteren Bereich der Kolonne höher ist als im oberen Bereich der Kolonne, mit einer Temperaturdifferenz zwischen dem oberen und dem unteren Bereich der Kolonne von 40°C bis 210°C.

Verfahren zur Herstellung von im wesentlichen Ameisensäure-freien N-Alkyl-N'-methylalkylenharnstoffen

Procedimiento para la obtencion de n-alquil-n'-metil-alquilenureas esencialmente exentas de acido formico.

Procedimiento para la obtención de N-alquil-N¿- metilalquilenureas de la fórmula con R1 = H o CH3, R2 = CnH2n+1 con n = 1-4 y x = 0 o 1, con un contenido en ácido fórmico en el producto final menor que el 0,1 %, a partir de las correspondientes alquilenureas mediante reacción con formaldehído monómero o polímero, en presencia de ácido fórmico, caracterizado porque la mezcla, obtenida en la reacción, constituida por N-alquil-N¿-metilalquilenurea y ácido fórmico se conduce a la parte superior de una columna de destilación, se destila sin otros aditivos y se retira por la parte inferior de la columna N-alquil-N¿- metilalquilenureas esencialmente exenta de ácido fórmico, ajustándose la presión en la zona superior de la columna a un valor mayor que en la zona inferior de la columna y la diferencia de presión entre la zona superior y la zona inferior de la columna es de 10 hasta 100 mbares y se ajusta la temperatura en la zona inferior de la columnaa un valor mayor que en la zona superior de la columna, con una diferencia de temperatura entre la zona superior y la zona inferior de la columna de 40ºC hasta 210ºC.

制备基本上无甲酸的n－烷基－n′－甲基亚烷基脲的方法

本发明涉及一种在甲酸存在下，通过由相应的亚烷基脲与单或多聚甲醛反应制备下式所示的基本上无甲酸的N-烷基-N’-甲基亚烷基脲的方法，式中各基团的定义如说明书所述，该方法包括：将反应所得的N-烷基-N’-甲基亚烷基脲和甲酸的混合物送至蒸馏塔的上部，不附加额外步骤进行蒸馏，并在蒸馏塔的下部排出基本上无甲酸的N-烷基-N’-甲基亚烷基脲，设定反应参数使得塔上部的压力高于塔下部的压力，塔上下两部的压力差为10～100毫巴；塔下部的温度高于塔上部的温度，塔上下两部的温度差为40℃～210℃。

Method for producing derivatives of hexahydropyrimidine and converting the same to 1, 3-diamines

Dialkylaminoethyl ester salts of cyclic guanidino acids and their preparation

Verfahren zur herstellung von cyclischen n,n'dimethylharnstoffen.

[UNK]

Bacteriostatic complexes of silver salts and substituted tetrahydropyrimidine-2-thiones and hexahydropyrimidine-2-thiones

[UNK]

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一种1,3-二甲基丙撑脲的连续化制备方法

一种1,3‑二甲基丙撑脲的连续化制备方法，其属于有机合成领域。该方法以丙烯脲为原料，以甲醛、甲酸为甲基化试剂，在一定的温度和压力下，通过微通道反应器进行甲基化反应，经减压浓缩，得到1,3‑二甲基丙撑脲。本发明提供一种1,3‑二甲基丙撑脲的连续化制备工艺方法，整个反应体系实现智能连续化，制备方法简单，反应时间较短，产品收率达到75‑80%，提高产能。

2-amino-imidazol-2-ine derivatives

5,5-disubstituierte 4-carbamido-hexahydropyrimidine und verfahren zur herstellung von 5,5-disubstituierten 4-carbamido- hexahydropyrimidinen

Verfahren zur herstellung von 5,5- disubstituierten 4-ureido-hexyhadropyrimidinen

Verfahren zur Herstellung von 2-Oxo-hexahydropyrimidinen

Verfahren zur herstellung von cyclischen n,n'-dimethylharnstoffen.

Preparation of cyclic N,N'-dimethylureas

Cyclic N,N'-dimethylureas are prepared by catalytic hydrogenation of a cyclic urea which carries hydroxyl groups in the α-position to the two nitrogen atoms.

Hexahydropyrimidyl-(4)-aether und verfahren zu ihrer herstellung

[UNK]

Verfahren zur Herstellung von cyclischen Harnstoffderivaten

Verfahren zur Herstellung von Propylenharnstoffaldehyden

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Verfahren zur Herstellung von Tetrahydro-2-(1H)-Pyrimidon

Manufacture of tetrahydro-2-(1h)-pyrimidinone

一种洛匹那韦衍生物的制备方法

本发明公开了一种洛匹那韦衍生物的制备方法，属于化合物制备领域，提供了一种工艺设计合理、产率高、操作过程方便可控的新型药物分子洛匹那韦衍生物的合成方法。本发明以胺基保护的环氧丙胺和羧基保护的L‑缬氨酸为原料，通过七步反应，实现洛匹那韦衍生物的合成。本发明提供的制备方法工艺设计合理、可操作性强、反应条件比较温和、产率高。本发明制备得到的洛匹那韦衍生物对洛匹那韦进行质量、安全性和效能科学评价提供了重要依据。同时相较于洛匹那韦，本发明合成的一种洛匹那韦衍生物有更好的水溶性，克服了洛匹那韦本身较低的水溶性，洛匹那韦的口服生物利用度较差的弱点，可开发成为洛匹那韦的替代品。

Hexahydropyrimidin-(4)-yl-ethers and process for their preparation

一种1,3-二甲基丙撑脲的连续化制备方法

一种1,3‑二甲基丙撑脲的连续化制备方法，其属于有机合成领域。该方法以丙烯脲为原料，以甲醛、甲酸为甲基化试剂，在一定的温度和压力下，通过微通道反应器进行甲基化反应，经减压浓缩，得到1,3‑二甲基丙撑脲。本发明提供一种1,3‑二甲基丙撑脲的连续化制备工艺方法，整个反应体系实现智能连续化，制备方法简单，反应时间较短，产品收率达到75‑80%，提高产能。

Préparation de la tétrahydro-2-(1eta)-pyrimidinone

一种洛匹那韦的新晶型及其制备方法

本发明适用于药物化学领域，提供了一种洛匹那韦的新晶型及其制备方法；所述的新晶型的X射线粉末衍射图中在2θ为5.179°±0.02°、7.508°±0.02°、9.235°±0.02°、10.532°±0.02°、12.015°±0.02°、14.475°±0.02°、16.154°±0.02°、18.123°±0.02°的位置处有特征峰。新晶型样品的X‑射线衍射图具有特征性，经过红外光谱，HPLC和DSC证实洛匹那韦在晶型转变后并未发生化学结构的变化，且在热力学、化学稳定性上均有显著提高。同时本发明提供了所述新晶型的制备方法，该方法在实现上简单、高效，回收率高，适用于大批量的工业化生产。

一种洛匹那韦衍生物的制备方法

本发明公开了一种洛匹那韦衍生物的制备方法，属于化合物制备领域，提供了一种工艺设计合理、产率高、操作过程方便可控的新型药物分子洛匹那韦衍生物的合成方法。本发明以胺基保护的环氧丙胺和羧基保护的L‑缬氨酸为原料，通过七步反应，实现洛匹那韦衍生物的合成。本发明提供的制备方法工艺设计合理、可操作性强、反应条件比较温和、产率高。本发明制备得到的洛匹那韦衍生物对洛匹那韦进行质量、安全性和效能科学评价提供了重要依据。同时相较于洛匹那韦，本发明合成的一种洛匹那韦衍生物有更好的水溶性，克服了洛匹那韦本身较低的水溶性，洛匹那韦的口服生物利用度较差的弱点，可开发成为洛匹那韦的替代品。

一种洛匹那韦的制备方法

本发明提供式Ⅰ所示的制备方法，（2S）‑N‑{（1S，3S，4S）‑1‑苄基‑4‑［2‑（2,6‑二甲基苯氧基）乙酰氨基］‑3‑羟基‑5‑苯基戊基}‑3‑甲基‑2‑（2‑氧代四氢嘧啶‑1‑基）丁酰胺的制备方法。

一种洛匹那韦新晶型及其制备方法

本发明公开了一种洛匹那韦新晶型及其制备方法，涉及药物晶型技术领域，本发明制备了洛匹那韦并培养出洛匹那韦新晶型，从得到的单晶结构中可以看到洛匹那韦分子中四个手性中心的真实立体结构，晶体数据首次被英国剑桥大学晶体数据库收录，CCDC 1969375，和目前报道的其他检测方法相比，X射线单晶衍射方法是确定洛匹那韦绝对构型和空间结构最直接和最直观的方法。

一锅法制备洛匹那伟

一锅法制备洛匹那伟(I)， 其由2,6‑二甲基苯氧基乙酸、羧基活化剂、式(III)所示化合物在有机溶剂中进行缩合反应