| abstract |
NEW MATERIAL:A halogenated PGI 2 shown by the formulaI(R 1 is H or 1W 10C alkyl; R 2 and R 3 are H or hydroxyl-protecting group, may be the same or different; X is halogen) or its nontoxic salt of its acid when R 1 is H. n EXAMPLE: (5E)-5-Chloro PGI 2 methyl ester-11,15-bis-t-butyl-dimethylsilyl ether. n USE: A drug having an inhibiting action on blood platelet aggregation, relaxing action on smooth muscle, hypotensive action, antiulcer action, suppressing action of cancer antasthmatic, etc. An intermediate for hapten or other PGI 2 simulants. n PROCESS: A 5-halo-Δ 6 -PGI 2 shown by the formula II (R 11 is 1W10C alkyl; R 21 and R 31 are hydroxyl-protecting group, may be the same or different; X is halogen) is isomerized in the presence of an acid catalyst, and, if necessary, the reaction product is deprotected and/or subjected to salt forming reaction, to give a compound shown by the formulaI. n COPYRIGHT: (C)1982,JPO&Japio |