15-alkylprostaglandins having improved activity

摘要

15-Alkylprostaglandins having improved activity. New cpds.: their mirror images and racemates (where X is tCH=CH, or CH2.CH2; Y and Z both = CH2.CH2 or when X = tCH=CH2 Y = C-CH=CH and Z = C-CH=CH or CH2CH2; A is 1-4C alkyl, 7-12C aralkyl or phenyl (opt. with 1 or 2 F, Cl or 1-4C alkyl); R2 is Et or Me; R3 is 1-8C alkyl or SiA3; R4 is H or 1-8C alkyl); (I) being intermediates for (II). (II) and (III) have greater activity than corresponding cpds. with R2 = H e.g. in reducing arterial press.; as smooth muscle contractants, antilipolytics, and gastric secretion and blood platelet coagulation inhibitors, etc. in both humans and animals. Prepn. is by oxidn. of cpd. (II) R2 = H to 15-oxo; silylation to (I); Grignard reaction/hydrolysis to (II), opt. followed by oxidn. to (III).