METHOD OF PREPARING 7-OXOPROSTACYCLINE DERIVATIVES

摘要

PCT No. PCT/EP81/00148 Sec. 371 Date May 17, 1982 Sec. 102(e) Date May 17, 1982 PCT Filed Sep. 17, 1981 PCT Pub. No. WO82/01002 PCT Pub. Date Apr. 1, 1982.Prostacyclin, although having a useful dilating effect on blood vessels, is not sufficiently stable to ensure successful use as a hypotensive agent. A 7-oxo prostacyclin derivative of the general formula (I) in which R1 represents the radical OR3 wherein R3 represents hydrogen, a straight-chain or branched optionally substituted, (C1-C10)alkyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heterocyclic, or R1 represents the radical NHR4 wherein R4 represents hydrogen, or a group derived from an unsaturated or saturated, unsubstituted or substituted, (C1-C15)organic carboxylic or sulphonic acid, A represents -CH2-CH2-, cis-CH=CH- or trans-CH=CH-, W represents either having a free or functionally modified hydroxy group which may be in the alpha - or beta -position, D and E together represent a direct bond, or D represents a straight-chain or branched, unsaturated or saturated, optionally substituted (C1-C10)alkylene, and E represents oxygen or a direct bond, R2 represents a straight-chain or branched optionally substituted, (C1-C10)alkyl, a straight-chain or branched optionally substituted, (C2-C10)alkenyl, or, where D and E together represent a direct bond, a straight-chain or branched optionally substituted (C2-C6)alkynyl, and R5 represents a free or functionally modified hydroxy group, has proved to have not only a hypotensive and bronchodilative action, for example, but also an increased stability over prostacyclin. Advantages in medicinal use over other prostaglandins have also been found.