| abstract |
NEW MATERIAL:A carbacyclin derivative of formula I (Z is -COOH, -CONH 2 or -CH 2 OH; A is -CH=CH- or -C≡C-; B is (substituted) indanyl, (substituted) benzodioxanyl, (substituted) benzodioxolanyl or 2,3,5,6,7,8- hexahydrobenzodioxolanyl) or its alkali addition salt. n EXAMPLE: 15α-hydroxy-15-(benzodioxan-6-yl)carbacyclin. n USE: It has antiulcer, anticoagulation and vasodilating activities and is useful as a drug. It has high chemical stability. n PREPARATION: A compound of formula II (R 1 is lower alkyl; R 2 is hydroxyl protecting group) is made to react with a compound of formula III (Y is H or halogen) and the resultant compound of formula IV is reduced to obtain a compound of formula V. The product is subjected to dehydrohalogenation reaction when Y is halogen and to deprotection reaction of OH group and COOH group to obtain a compound of formula I wherein A is triple bond. n COPYRIGHT: (C)1988,JPO&Japio |