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    • 92. 发明申请
    • PROCESSES FOR THE PREPARATION OF PYRROLE DERIVATIVES
    • 制备吡咯衍生物的方法
    • WO2006032959A2
    • 2006-03-30
    • PCT/IB2005/002348
    • 2005-08-05
    • GLENMARK PHARMACEUTICALS LIMITEDJOSHI, Narendra, ShriramBHIRUD, Shekhar, BhaskarDAMLE, Subhash, Vishwanath
    • JOSHI, Narendra, ShriramBHIRUD, Shekhar, BhaskarDAMLE, Subhash, Vishwanath
    • C07D207/34A61K31/40
    • C07D405/12Y02P20/55
    • A process for the preparation of a pyrrole derivative or a racemic mixture, an enantiomer, a diastereoisomer, a mixture thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof comprising reacting an amino compound of the general formula (I), wherein each R is independently hydrogen or a hydrolyzable protecting group, or each R, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group and R 1 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt, with a di-oxo compound of the general formula (II), wherein R 2 is 1-naphthyl, 2-naphthyl, a C 3- C 25 cycloalkyl group, norbornenyl, a substituted or unsubstituted aryl group, benzyl, 2-, 3-, or 4-pyridinyl, or 2-, 3-, 4-pyridinyl-N-oxide, R 3 and R 4 are independently hydrogen, a lower alkyl, a C 3- C 25 cycloalkyl group, a substituted or unsubstituted aryl group, cyano, trifluoromethyl, or -CONR 6 R 7 wherein R 6 and R 7 are independently hydrogen, a lower alkyl or a substituted or unsubstituted aryl group and R 5 is a lower alkyl, a C 3- C 25 cycloalkyl or trifluoromethyl; in the presence of a catalyst and in at least one solvent. Also disclosed is a process for hydrolyzing the pyrrole derivative to provide, for example, atorvastatin or pharmaceutically acceptable salts thereof.
    • 一种制备吡咯衍生物或外消旋混合物,对映体,非对映异构体,其混合物,其互变异构体或其药学上可接受的盐的方法,包括使通式(I)的氨基化合物与其中每个R 独立地是氢或可水解保护基,或者每个R与各自键合的氧原子一起形成可水解的环保护基,或者每个R与与每个氧原子键合的相同取代基键合,形成 可水解保护基和R
    • 93. 发明申请
    • PROCESS FOR THE PREPARATION OF DISUBSTITUTED ACETYLENES BEARING HETEROAROMATIC AND HETEROBICYCLIC GROUPS
    • 制备异构乙酰乙烯的方法,用于轴承异构体和环氧基团
    • WO2005123713A1
    • 2005-12-29
    • PCT/IB2005/001722
    • 2005-06-17
    • GLENMARK PHARMACEUTICALS LIMITEDKUMAR, Bobba, Venkata, SivaBHIRUD, Shekhar, BhaskarCHANDRASEKHAR, BatchuRAUT, Changdev, Namdev
    • KUMAR, Bobba, Venkata, SivaBHIRUD, Shekhar, BhaskarCHANDRASEKHAR, BatchuRAUT, Changdev, Namdev
    • C07D335/02
    • C07D335/06
    • A process for the preparation of a disubstituted acetylene bearing heteroaromatic and heterobicyclic groups of formula I is provided wherein X is S, O, or NR 1 wherein R 1 is hydrogen or a C 1 -C 6 straight or branched alkyl group; R is hydrogen or a C 1 -C 6 straight or branched alkyl group; A is a substituted or unsubstituted pyridinyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl group; n is 0-­4; and B is H 2 -COOH, -CH 2 OH, -CHO or a C 1 -C 6 alkyl acetal derivative, - COR 2 or a C 1 ­C6 alkyl ketal derivative where R 2 is -(CH 2 ),,,CH 3 where m is 0-4 or COOR 3 wherein R 3 is a straight or branched C 1 -C 30 alkyl group, a substituted or unsubstituted C 6 -C 30 aromatic group, a substituted or unsubstituted C 3 -C 30 cycloalkyl, a substituted or unsubstituted C 3 ­C 30 cycloalkylalkyl, a substituted or unsubstituted C 3 -C30 cycloalkenyl, a substituted or unsubstituted C 5 -C 30 aryl, a substituted or unsubstituted C 5 -C 30 arylalkyl, a substituted or unsubstituted C 5 -C 30 heteroaryl, a substituted or unsubstituted C 3 -C 30 heterocyclic ring, a substituted or unsubstituted C 4 -C 30 heterocyclylalkyl, a substituted or unsubstituted C 6 -C 30 heteroarylalkyl, the process comprising a Sonogashira coupling reaction between a compound of formula II wherein X and R have the aforestated meanings, with a compound of formula III wherein X' is a halogen and A, n and B have the aforestated meanings, in the presence of a base and a transition metal catalyst and in a polar aprotic solvent.
    • 提供制备具有式I的二取代乙炔的杂芳族和杂双环基团的方法,其中X是S,O或NR 1,其中R 1是氢或C 1 -C 6直链或支链烷基; R是氢或C 1 -C 6直链或支链烷基; A是取代或未取代的吡啶基,噻吩基,呋喃基,哒嗪基,嘧啶基或吡嗪基; n为0-4; 并且B是H 2 -COOH,-CH 2 OH,-CHO或C 1 -C 6烷基缩醛衍生物,-COR 2或C 1 -C 6烷基缩酮衍生物,其中R 2是 - (CH 2)n CH 3,其中m是0 -4或COOR 3,其中R 3是直链或支链C 1 -C 30烷基,取代或未取代的C 6 -C 30芳族基团,取代或未取代的C 3 -C 30环烷基,取代或未取代的C 3 -C 30环烷基烷基, 取代或未取代的C 3 -C 30环烯基,取代或未取代的C 5 -C 30芳基,取代或未取代的C 5 -C 30芳烷基,取代或未取代的C 5 -C 30杂芳基,取代或未取代的C 3 -C 30杂环,取代或未取代的C 4 -C30杂环基烷基,取代或未取代的C 6 -C 30杂芳基烷基,所述方法包括其中X和R具有上述含义的式II化合物之间的Sonogashira偶联反应与式III化合物,其中X'为卤素和A, n和b具有上述含义,在存在o f碱和过渡金属催化剂和极性非质子溶剂。