Prostaglandin i2 analog compound, its preparation, and pharmaceutical composition containing the same

Abstract

Abstract NEW MATERIAL:A compound of formula I [Y is ethylene, etc., R 1 is H, 1W12C alkyl, etc.; R 2 is H, methyl, etc.; R 3 is single bond or 1W5C alkylene; R 4 is H, 1W8C alkylene, etc.; A is single bond or O (when R 3 is not single bond, then R 4 is not H); wavy line represents α-configuration, β-configuration, etc.; the couble bond between the 4- and the 5-position carbon atoms is E, Z or EZ], its cyclodextrin clathrate compound, a non-toxic salt of the acid, or a non-toxic acid addition salt of the amine. EXAMPLE: ( 4EZ,13E )-( 9α,11α,15S )-5,9-epoxy-11,15-dihydroxyprosta-4,6,13-trienoic acid methyl ester. USE: Medicine effective to the remedy for arteriosclerosis, cardiac insufficiency, thrombosis, etc. PROCESS: The compound of formula I is prepared by the dehydrohalogenation reaction of a compound of formula II (X is Br or I; the absolute configuration of the 5- and the 6-position carbon stoms is S, R or RS) in an inert organic solvent such as benzene, at room temp. to 160°C. COPYRIGHT: (C)1981,JPO&Japio

Inventors

• 👤 Haniroku Miyake
• 👤 Hisao Nakai
• 👤 Nobuyuki Hamanaka
• 👤 Masaki Hayashi

Bibliographic Details