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    Process for the preparation of 20-keto-21 alpha-01-steroids
    44.
    发明授权
    Process for the preparation of 20-keto-21 alpha-01-steroids 失效
    制备20-keto-21α-01类固醇的方法

    公开(公告)号：US5399685A

    公开(公告)日：1995-03-21

    申请号：US75822

    申请日：1993-06-11

    申请人： Jean Buendia ,  Veronique Crocq ,  Christian Masson ,  Denis Prat ,  Michel Vivat

    发明人： Jean Buendia ,  Veronique Crocq ,  Christian Masson ,  Denis Prat ,  Michel Vivat

    IPC分类号： C07J9/00 ,  C07J21/00 ,  C07J33/00 ,  C07J41/00 ,  C07J75/00 ,  C12P33/00 ,  C12R1/865

    CPC分类号： C07J9/00 ,  C07J21/006 ,  C07J33/007 ,  C07J41/0094

    摘要： A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, R.sub.3 is alkyl of 1 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.4 is a remainder of an easily cleavable ether, K is a protected ketone function in the form of ketal, thioketal or mixed ketal and R.sub.1 has the above definition with a magnesium organic compound reagent of the formulaHalMg--CH.sub.2 --R.sub.2 Awherein Hal is a halogen and R.sub.2 is defined as above to obtain a compound of the formula ##STR3## wherein R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an acylation agent to obtain a compound of the formula ##STR4## wherein R.sub.5 is alkyl of 1 to 6 carbon atoms or aryl of 6 to 10 carbon atoms and R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an appropriate alkylation agent to obtain a compound of the formula ##STR5## wherein R.sub.1, R.sub.2, R.sub.3 and K are defined as above, subjecting the latter to autoxidation to obtain a compound of the formula ##STR6## wherein R.sub.1, R.sub.2, R.sub.3 and K are defined as above, reacting the latter with an acid to obtain a reconjugated 3-keto compound of the formula ##STR7## wherein R.sub.1, R.sub.2 and R.sub.3 are defined as above and reacting the latter with a regio- and enantioselective reducing agent to obtain a compound of formula I and intermediates formed therein.

    摘要翻译： 一种制备式I化合物的方法，其中R 1是1至3个碳原子的烷基，R 2是1至12个碳原子的烷基，R 3是1至4个碳原子的烷基，包括使 其中R 4是易裂解醚的剩余部分，K是缩酮形式，缩醛缩醛或混合缩酮形式的被保护酮官能团，并且R 1具有上述定义与式HalMg- CH2-R2A其中Hal是卤素，R2如上定义，得到式III的化合物，其中R 1，R 2和K如上定义，使其与酰化剂反应，得到式 其中R 5是1至6个碳原子的烷基或6至10个碳原子的芳基，并且R 1，R 2和K如上定义，使其与适当的烷基化剂反应，得到下式的化合物：IMAGE > V其中R1，R2，R3和K如上所定义，对其进行处理 进行自氧化以获得式VI的化合物，其中R 1，R 2，R 3和K如上定义，使其与酸反应，得到下式的共轭3-酮化合物，其中R 1， R2和R3如上定义并使其与区域和对映选择性还原剂反应，得到式I化合物及其中形成的中间体。

    Novel 23-keto-steroids
    45.
    发明授权
    Novel 23-keto-steroids 失效
    新型23-酮类固醇

    公开(公告)号：US4927921A

    公开(公告)日：1990-05-22

    申请号：US128997

    申请日：1987-12-04

    申请人： Michel Vivat ,  Jean Buendia

    发明人： Michel Vivat ,  Jean Buendia

    IPC分类号： C07J9/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00

    CPC分类号： C07J9/005 ,  C07J31/006 ,  C07J43/003

    摘要： A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, and A,B,C and D rings optionally containing at least one double bond and optionally substituted with at least one member of the group consisting of optionally protected --OH, .dbd.O, alkyl and alkoxy of 1 to 4 carbon atoms, halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkylthio and alkoxy of 1 to 6 carbon atoms, aralkoxy, arylthio and aralkylthio of 7 to 15 carbon atoms and ##STR2## R.sub.3 and R.sub.4 are individually hydrogen, or alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 15 carbon atoms or taken together with the nitrogen form a heterocycle optionally containing another nitrogen or oxygen atom, excepting the product in which R is methoxy, R.sub.1 and R.sub.2 each represent methyl, A ring carries a 3.beta.-acetoxy function and B ring contains a double bond in 5(6) useful as intermediates for the preparation of 20-keto-pregnanes.

    摘要翻译： 式I的化合物，其中R 1是氢或甲基，R 2是甲基或乙基，A，B，C和D环任选地含有至少一个双键并且任选被至少一个成员所取代 任选保护的-OH，= O，1-4个碳原子的烷基和烷氧基，2至4个碳原子的卤素和烯基和炔基，R选自卤素，-OH，烷硫基和烷氧基， 6个碳原子，7至15个碳原子的芳烷氧基，芳硫基和芳烷硫基，而R 3和R 4分别是氢或1至6个碳原子的烷基或7至15个碳原子的芳烷基或与氮一起形成 任选地含有另外的氮或氧原子的杂环，除了其中R是甲氧基的产物，R1和R2各自表示甲基，A环带有3β-乙酰氧基官能团，并且B环在5（6）中含有双键，可用作中间体 20-酮 - 孕烷的制备。

    Novel steroids
    46.
    发明授权
    Novel steroids 失效
    新型类固醇

    公开(公告)号：US4847014A

    公开(公告)日：1989-07-11

    申请号：US129658

    申请日：1987-12-07

    申请人： Michel Vivat ,  Jean Buendia

    发明人： Michel Vivat ,  Jean Buendia

    IPC分类号： C07J7/00 ,  C07J9/00 ,  C07J31/00 ,  C07J41/00

    CPC分类号： C07J31/006 ,  C07J41/0061 ,  C07J7/002 ,  C07J9/005

    摘要： A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, the A,B,C and D rings optionally have one or more double bonds and are optionally substituted with one or more members of the group consisting of halogen protected hydroxy, 1/8O, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkoxy of 1 to 6 carbon atoms, aralkoxy of 7 to 15 carbon atoms, alkylthio of 1 to 6 carbon atoms, arylthio of 6 to 14 carbon atoms, aralkylthio of 7 to 15 carbon atoms and ##STR2## wherein R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and aralkyl of 7 to 15 carbon atoms or R.sub.3 and R.sub.4 together with the nitrogen atom form another heterocycle optionally containing a nitrogen atom or oxygen atom and their preparation and their use to form 20-keto-pregnanes.

    摘要翻译： 式Ⅰ化合物，其中R 1是氢或甲基，R 2是甲基或乙基，A，B，C和D环任选地具有一个或多个双键并且任选被一个或多个基团的成员取代 由卤素保护的羟基，1/80，烷基和1至4个碳原子的烷氧基和2至4个碳原子的烯基和炔基组成，R选自卤素，-OH，1至6个碳原子的烷氧基 具有7至15个碳原子的芳烷氧基，1至6个碳原子的烷硫基，6至14个碳原子的芳硫基，7至15个碳原子的芳烷硫基和其中R 3和R 4分别选自氢， 1至6个碳原子的烷基和7至15个碳原子的芳烷基或R3和R4与氮原子一起形成任选含有氮原子或氧原子的另一个杂环及其制备及其用于形成20-酮 - 孕烷的用途。

    Process for the production of prednisone 17.21-diacylates
    47.
    发明授权
    Process for the production of prednisone 17.21-diacylates 失效
    生产泼尼松17.21-二酰基化酶的方法

    公开(公告)号：US4601854A

    公开(公告)日：1986-07-22

    申请号：US695485

    申请日：1985-01-28

    申请人： Jean Buendia ,  Michel Vivat

    发明人： Jean Buendia ,  Michel Vivat

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J41/00 ,  C07J43/00 ,  C07J21/00

    CPC分类号： C07J9/00 ,  C07J41/005 ,  C07J43/006 ,  C07J5/0053 ,  C07J7/0015 ,  C07J7/0085

    摘要： A novel process for the preparation of prednisone derivatives of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 8 carbon atoms comprising reacting a compound of the formula ##STR2## with a reducing agent to obtain a compound of the formula ##STR3## reacting the latter with a strong base in the presence of copper ions and oxygen to obtain a compound of the formula ##STR4## reacting the latter with hydroxylamine to obtain a compound of the formula ##STR5## in its syn or anti isomeric form or a mixture thereof, reacting the latter with an acylating agent derived from a radical of the formula ##STR6## and with a reducing agent to obtain a compound of the formula ##STR7## in its Z or E isomeric form or a mixture thereof, subjecting the latter to treatment with an epoxidizing agent and then a dehydrating agent to obtain a compound of the formula ##STR8## reacting the latter with a halogenation agent and subjecting the resulting product to hydrolysis to obtain a compound of the formula ##STR9## wherein Hal is a halogen and reacting the latter with a derivative of an acyl of the formula R.sub.1 CO-- to obtain the compound of formula I which are known compounds.

    摘要翻译： 一种用于制备式I的泼尼松衍生物的新方法，其中R 1是1至4个碳原子的烷基，R 2选自氢和1至8个碳原子的烃，包括使 式II的化合物与还原剂反应，得到下式的化合物，其中在后者与强碱在铜离子和氧的存在下反应，得到下式的化合物，其中IV与式 羟胺以获得其顺式或反式异构体形式的式VIII化合物或其混合物，使其与衍生自下式基团的酰化剂和还原剂反应，得到化合物 其Z或E异构体形式的式（VI）化合物或其混合物，将其用环氧化物处理，然后用脱水剂处理，得到式 脱色剂并将所得产物水解，得到式VIII的化合物，其中Hal为卤素并使其与式R 1 CO-的酰基衍生物反应，得到已知的式I化合物 化合物。

    Method of imparting a pleasant odor
    48.
    发明授权
    Method of imparting a pleasant odor 失效
    赋予气味的方法

    公开(公告)号：US4521331A

    公开(公告)日：1985-06-04

    申请号：US438486

    申请日：1982-11-02

    申请人： Jacques Martel ,  Jean Buendia ,  Francois Nezot

    发明人： Jacques Martel ,  Jean Buendia ,  Francois Nezot

    IPC分类号： C07C69/003 ,  A61K8/37 ,  A61Q13/00 ,  C07C67/00 ,  C07C69/007 ,  C07C253/00 ,  C07C255/17 ,  C07C255/46 ,  C07C255/57 ,  C07D207/00 ,  C07D213/79 ,  C07D213/80 ,  C07D307/54 ,  C07D307/64 ,  C07D307/68 ,  C07D333/24 ,  C07D333/32 ,  C11B9/00 ,  A61K7/16 ,  C11D3/50

    CPC分类号： C11B9/003 ,  C07D333/32

    摘要： All possible isomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of alkyl of 1 to 8 carbon atoms and alkenyl of 2 to 8 carbon atoms and R is selected from the group consisting of (a) hydrogen, (b) alkyl of 1 to 12 carbon atoms and alkenyl and alkynyl of 2 to 12 carbon atoms optionally substituted with cyano, saturated or unsaturated cycloalkyl or bicycloalkyl of 3 to 12 carbon atoms also optionally substituted, and optionally interrupted by an oxygen atom or containing a keto group, (c) cycloalkyl of 3 to 12 carbon atoms optionally having at least one double bond and at least one alkyl substituent of 1 to 4 carbon atoms, (d) aryl, arylalkyl, aralkenyl and aralkynyl of 6 to 20 carbon atoms optionally substituted on the aryl ring and the alkyl, alkenyl or alkynyl being optionally interrupted with an oxygen or containing a ketone group and (e) heteroaryl, heteroaralkyl, heteroaralkenyl and heteroaralkynyl optionally substituted on the heteroaryl ring and the alkyl, alkenyl and alkynyl being optionally interrupted with an oxygen atom or having a keto group with the proviso that R is not methyl when R.sub.1 is 2-methyl-1-propenyl, useful as perfume agents.

    摘要翻译： 式Ⅰ化合物的所有可能的异构体形式及其混合物，其中R 1选自1至8个碳原子的烷基和2至8个碳原子的链烯基，R选自 （a）氢，（b）1至12个碳原子的烷基和2至12个碳原子的烯基和炔基，其任选被氰基，3至12个碳原子的饱和或不饱和环烷基或双环烷基取代，也可任选地被 氧原子或含有酮基，（c）任选具有至少一个双键和至少一个碳原子数为1至4的烷基取代基的碳原子数为3至12的环烷基，（d）芳基，芳基烷基，芳烯基和芳炔基 任选在芳基环上被取代的碳原子数6〜20个，烷基，链烯基或炔基任选被氧或含有酮基中断，和（e）杂芳基，杂芳烷基，杂链烯基和杂炔基任选地 在杂芳基环上被取代，并且烷基，烯基和炔基任选被氧原子中断或具有酮基，条件是当R 1是2-甲基-1-丙烯基时，R不是甲基，可用作香料剂。

    Epimerization of trans chrysanthemates
    49.
    发明授权
    Epimerization of trans chrysanthemates 失效
    反式菊花异构化

    公开(公告)号：US4447637A

    公开(公告)日：1984-05-08

    申请号：US347278

    申请日：1982-02-09

    申请人： Jacques Martel ,  Jean Buendia ,  Jeanine Nierat

    发明人： Jacques Martel ,  Jean Buendia ,  Jeanine Nierat

    IPC分类号： C07C69/747 ,  C07C51/353 ,  C07C51/487 ,  C07C61/04 ,  C07C61/37 ,  C07C67/333 ,  C07C69/74 ,  C07C61/18

    CPC分类号： C07C61/37 ,  C07C51/353 ,  C07C51/487

    摘要： A novel process for the epimerization of alkyl trans chrysanthemates comprising reacting at a low temperature in an anhydrous organic solvent an alkyl trans chrysanthemate of the formula ##STR1## of the 1S, trans or 1R, trans configuration wherein R is alkyl of 1 to 6 carbon atoms with a strong alkali metal base to obtain a compound of the formula ##STR2## wherein R has the above definition and M is an alkali metal, reacting the latter compound with a reactant of the formulaY--Awherein A is selected from the group consisting of chlorine, bromine, iodine and anion derived from a hydrogen acid and Y is an organic radical capable of forming a ketal of a ketene to obtain a compound of the formula ##STR3## reacting the latter at a low temperature in an anhydrous organic solvent with a proton donor to obtain a mixture of the corresponding alkyl cis chrysanthemate and alkyl trans chrysanthemate and recovering the cis chrysanthemic acid of the formula ##STR4## with the 1R, cis or 1S, cis configuration.

    摘要翻译： 一种用于烷基反式菊氨酸差向异构化的新方法，其包括在低温下在无水有机溶剂中反应1S，反式或1R，反式构型的式II的烷基反式菊酯，其中R是1至6的烷基 具有强碱金属碱的碳原子以得到式III的化合物，其中R具有上述定义，M是碱金属，使后一化合物与式YA的反应物反应，其中A选自 由氯，溴，碘和由氢酸衍生的阴离子组成，Y是能够形成乙烯酮缩酮的有机基团，得到下式的化合物，其中IV在低温下与无水有机物 溶剂与质子供体反应，得到相应的顺式菊酸菊酯和反式菊酸酯的混合物，并用1R，顺式或1S的方法回收式Ⅰ的顺式菊酸， 顺式配置。

    .beta.-Lactones of 2-hydroxy-cyclopentanecarboxylic acid
    50.
    发明授权
    .beta.-Lactones of 2-hydroxy-cyclopentanecarboxylic acid 失效
    β-内酯2-羟基 - 环戊烷羧酸的内酯

    公开(公告)号：US4221809A

    公开(公告)日：1980-09-09

    申请号：US36877

    申请日：1979-05-08

    申请人： Jean Buendia ,  Michel Vivat

    发明人： Jean Buendia ,  Michel Vivat

    IPC分类号： C07C62/32 ,  C07D305/14 ,  C07D309/12 ,  A61K31/365

    CPC分类号： C07D309/12 ,  C07C62/32 ,  C07D305/14

    摘要： Novel lactones of the formula ##STR1## wherein the dotted line indicates the optional presence of a second bond, A is a single bond or --CH.sub.2 --CH.sub.2 --, R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.6 is --OR'.sub.A, R'.sub.A is selected from the group consisting of hydrogen, tetrahydropyranyl, alkyl of 1 to 3 carbon atoms and ##STR2## R".sub.A is selected from the group consisting of alkyl of 1 to 3 carbon atoms optionally substituted with carboxyl and phenyl optionally substituted with a member of the group consisting of carboxyl, free hydroxyl, hydroxyl protected with an acyl of 2 to 4 carbon atoms and hydroxyl protected with an easily hydrolyzable group and R and R.sub.6 together form a keto group, R.sub.7 is --(CH.sub.2)m.sub.A --CH.sub.3, m.sub.A is 3,4,5 or 6 and R.sub.6 and R.sub.7 taken together form .dbd. CH--(CH.sub.2)n.sub. A --CH.sub.3 n.sub.A is 2,3,4 or 5 and the wavy lines indicate that the bonds are in one or the other of the possible configurations and when A is a simple bond, the bond between the cyclopentane ring and the oxygen is in the .alpha.-position having hypotensive activity and novel processes and intermediates for their preparation.

    摘要翻译： 具有式“IMAGE”I的新型内酯，其中虚线表示任选存在第二键，A是单键或-CH 2 -CH 2 - ，R选自氢，1至4的烷基 碳原子和2至4个碳原子的烯基和炔基，R6是-OR'A，R'A选自氢，四氢吡喃基，1至3个碳原子的烷基，并且R“A是 选自由任选被羧基取代的1至3个碳原子的烷基和任选被羧基，游离羟基，被2至4个碳原子的酰基保护的羟基和任选被羟基保护的羟基任选取代的苯基 易于水解的基团，R和R6一起形成酮基，R7是 - （CH2）mA-CH3，mA是3,4,5或6，R6和R7一起形成= CH-（CH 2）n A-CH 3 nA 是2,3,4或5，波浪线表示这些键处于一个或另一个可能的配置，当A是一个简单的波 nd，环戊烷环和氧之间的键位于具有低血压活性的α位和用于制备的新方法和中间体。