NEW MATERIAL:The compound of formulaI[R1 is H, 1W10C alkyl, 5W6-membered cycloaliphatic group, phenyl, etc.; R2 and R3 are H, tri(1W6C hydrocarbon) silyl group, etc.; R4 is H or methyl; R5 is 5W6C alkyl or 5W6-membered cycloaliphatic group; n is 1W2; the figure of formula II is ethylene or vinylene].
EXAMPLE: 20-Methyl-4-nor-7-thiaprostaglandin E1.
USE: It has prostaglandin-like activities such as blood platelet coagulation inhibiting activity, vasodilating activity, etc., and is useful as a preventive and remedy for thrombosis, an agent for inhibiting the coagulation of blood platelet, a hypotensive agent, etc.
PROCESS: The compound of formulaIcan be prepared by the conjugated addition reaction of the 2-organothio-2-cyclopentenone compound of formula III [R11 is 1W10C alkyl, etc.; R21 is tri(1W6C hydrocarbon)silyl] with the organocopper- lithium compound of formula IV (Y is halogen, etc., m is 1W2) in an aprotic organic solvent, followed by the elimination of the protecting group and/or hydrolysis of the product.
HASATO ATSUO
KUROZUMI SEIJI
| JPS5368753A | 1978-06-19 |
Next Patent: NOVEL 13,14-DIHYDRO-7-THIAPROSTAGLANDIN E1 AND ITS PREPARATION