Process for production of prostaglandins E or F, and novel 7-(thiocarbo-acyloxy) prostaglandins E or F
申请人:TEIJIN LIMITED
公开号:EP0103445A2
公开(公告)日:1984-03-21
A novel process for the production of prostaglandins E or F which comprises subjecting a 7-(thio-carboacyloxy)prostaglandin to selective deoxygenation reaction to split off the 7-(thioacyloxy) group, and thereafter, as required, subjecting the reaction product to reduction, deprotection and/or hydrolysis.
The present invention also provide a 7-(carboacyloxy or thiocarboacyloxy)prostaglandin E or F represented by the formula:
wherein
R1 represents H, C1-10 alkyl, or tri(C1-7 hydrocarbon)silyl,
R2 represents a C1-1 alkyl 5- or 6-membered cycloalkyl which may be substituted,
R5 represents H or CH3, each of R3 and R4 is H, OH or a protected hydroxyl, the symbol .... represents a single or double bond,
A represents
or
,
B represents -CH2CH2, -CH=CH- or -C≡C-, and
Z represents carboacyl or thiocarboacyl.
一种生产前列腺素E或F的新工艺,包括将7-(硫代羧基)前列腺素进行选择性脱氧反应,使7-(硫代羧基)基团分离,然后根据需要将反应产物进行还原、脱保护和/或水解。
本发明还提供由式表示的 7-(羧基或硫代羧基)前列腺素 E 或 F:
式中
R1 代表 H、C1-10 烷基或三(C1-7 烃)硅基、
R2 代表可被取代的 C1-1 烷基 5 或 6 元环烷基、
R5 代表 H 或 CH3,R3 和 R4 各为 H、OH 或受保护的羟基,符号 .... 代表单键或双键、
A 代表
或
,
B 代表-CH2CH2、-CH=CH- 或-C≡C-,以及
Z 代表羧基或硫代羧基。