申请人:SYNTEX (U.S.A.) INC.
公开号:EP0373612A2
公开(公告)日:1990-06-20
This invention relates to a novel process for making an allenic prostanoic acid derivative in the form of a single stereoisomer, or a mixture of stereoisomers, represented by the formula (I):
wherein R is lower alkyl, R¹ is a protecting group which can be selectively removed in the presence of R², R² is an acid-labile, base-stable protecting group, X is -(CH₂)₂- , trans -CH=CH- or -C≡C-, Y is -C(R³)(OR²)CH₂-, in which -OR² is in the α or β configuration and R³ is hydrogen or methyl, Z is alkyl, or phenyl, benzyl or phenoxy each optionally substituted on the phenyl ring, and the wavy lines represent the α or β configuration with the proviso that when one wavy line is α the other is β.
本发明涉及一种新工艺,用于制造由式(I)表示的单一立体异构体或立体异构体混合物形式的异链前列酸衍生物:
其中 R 是低级烷基,R¹ 是在 R² 存在下可选择性去除的保护基团,R² 是耐酸碱稳定的保护基团,X 是-(CH₂)₂- ,反式-CH=CH- 或-C≡C-,Y 是-C(R³)(OR²)CH₂-、其中,-OR² 为 α 或 β 构型,R³ 为氢或甲基,Z 为烷基或苯基、苄基或苯氧基,每个苯基环上均可选被取代,波浪线代表 α 或 β 构型,但当一条波浪线为 α 时,另一条波浪线为 β。