| abstract |
NEW MATERIAL:A 7-hydroxy PGI 2 shown by the formula I(R 1 is H, or 1W10C alkyl; K 2 and R 3 are H or OH-protecting group) or its acid addition salt where R 1 is H. n EXAMPLE: 7-Hydroxyl-PGI 2 methyl ester 11, 15-bis t-butyldimethyl-silyl ether. n USE: A hypotensor and an inhibitor for blood platelet aggregation, having improved stability and action selectivity as a drug of PGI 2 . n PROCESS: A compound shown by the formula II(R" is 1W10C alkyl) wherein preferably a steric configuration of 5-position is (R)-configuration, Δ 6 -double bond is (Z)-configuration, and a steric configuration of 7-position is (S) configuration is treated with a sulfurphilic compound, preferably an amine or a phosphorous type compound, and, if necessary, the resulting compound is subjected to a protective group removing reaction, a salt-forming reaction and/or a protecting reaction, to give a compound shown by the formulaIor a pharmaceutically acceptable salt of its acid. n COPYRIGHT: (C)1982,JPO&Japio |