发明名称 PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS
摘要 Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer:;wherein;R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.
申请公布号 US2015336921(A1) 申请公布日期 2015.11.26
申请号 US201514801966 申请日期 2015.07.17
申请人 CHIROGATE INTERNATIONAL INC. 发明人 Wei Shih-Yi;Yeh Yu-Chih;Hsu Min-Kuan;Kao Li-Ta
分类号 C07D309/12;C07F7/18;C07C51/347;C07C67/10;C07D407/14;C07D313/00 主分类号 C07D309/12
代理机构 代理人
主权项 1. A process for the purification of the compound of Formula IV: wherein  or a protecting group for carbonyl group; P1 and P2 are independently protecting groups for hydroxyl groups; is a single or double bond; R2 is a single bond or a C1-4-alkylene or —CH2O—; and R3 is a C1-7-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C1-4-alkyl, a halogen or a trihalomethyl; and X is OH, OR6, or NR4R5 wherein R4 and R6 are independently C1-7-alkyl, and R5 is H or C1-7-alkyl, comprising the steps of: (1) macrolactonization of a compound of Formula IV-1 containing 0˜5% 5,6-trans isomer or other stereoisomers: wherein  or a protecting group for carbonyl group and , P1, P2, R2 and R3 are as defined above, to form a compound of Formula III and unmacrolactonization isomers of the compound of Formula IV-1 or its derivative: wherein  , P1, R2 and R3 are as defined above, (2) removing the unmacrolactonization isomers of the compound of Formula IV-1 or its derivative, and (3) opening the macrolactone ring of the compound of Formula III by hydrolysis, transesterification or amidation to form a compound of Formula IV.
地址 YANGMEI CITY TW