| abstract |
NEW MATERIAL:The fluoro-PGI 2 compound of formulaI(R 1 is H or 1W10C alkyl; R 2 and R 3 are H or OH-protecting group; R 4 is F and R 5 and R 6 together represent a single bond, or R 6 is F and R 4 and R 5 together represent a single bond) or when R 1 is H, the non-toxic salt of the acid. n EXAMPLE: 7-Fluoro-PGI 2 methyl ester 11,15-diacetate. n USE: The compound exhibits blood platelet coagulation suppressing action, hypotensive action, smooth muscle relaxing action, etc., and is expected to be a drug. The compound having protected OH group is useful also as an intermediate of other compounds. n PROCESS: The compound of formulaIcan be prepared, e.g. by reacting 7-hydroxy- PGI 2 compound of formula II (R 11 is 1W10C alkyl; R 21 and R 31 are OH-protecting group) with the dialkylaminosulfate trifluoride of formula III (R 7 and R 8 are 1W5C alkyl, or R 7 and R 8 may together form a ring through a single bond or 0), and if necessary, eliminating the protecting group or hydrolyzing the product. n COPYRIGHT: (C)1982,JPO&Japio |