Processes and intermediates for thromboxane receptor antagonists.

摘要

Disclosed herein is a process for preparing a monoacyl of the formula <CHEM> 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)-R<1> 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 acyl-aldehydes, which are hydrolyzed with an alkali metal carbonate, bicarbonate or hydroxide to the cis furanol. The thromboxane receptor antagonist [1S-[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.