PROCESSES AND INTERMEDIATES FOR THROMBOXANE RECEPTOR ANTAGONISTS

摘要

HA528 PROCESS AND INTERMEDIATES FOR THROMBOXANE RECEPTOR ANTAGONISTS Disclosed herein is a process for preparing a monoacyl of the formula in which the associated diacyl is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the -O-C-(O)-R1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. This acyl-alcohol is oxidized to the associated acylaldehydes, which are hydrolyzed with an alkali metal carbonate, bicarbonate or hydroxide to the cis furanol. The thromboxane receptor antagonist ¢lS-¢1.alpha.,2.alpha.(Z),3.alpha.,4.alpha.!!-7-¢3¢¢¢¢(1-oxoheptyl)-amino!acetyl!amino!methyl-7-oxabicyclo-¢2.2.1!-hept-2-yl!-5-heptenoic acid may be prepared using these processes.