NOVEL THIAPROSTAGLANDIN E1 DERIVATIVES, PROCESS FOR PRODUCTION THEREOF, AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS

摘要

A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E1 derivatives of the formula (I). (I) wherein A represents -CH2- or in which n is 0, 1 or 2, provided that only one A cut of three is R1-R7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E1 derivatives, the enatiomers of said thiaprostaglandin E1 derivatives or their 15-epimers, and mixtures of these compounds. A 7-thiaprostaglandin E1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E1 derivative and/or its optical isomer may be prepared by subjecting an alpha , beta -unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII). Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.