Processes and intermediates for thromboxane receptor...

C - Chemistry – Metallurgy – 12 – P

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C12P 17/04 (2006.01) C07D 493/08 (2006.01) C07D 493/18 (2006.01) C12P 17/18 (2006.01) C12P 41/00 (2006.01)

Patent

CA 2055572

HA528 Abstract PROCESS AND INTERMEDIATES FOR THROMBOXANE RECEPTOR ANTAGONISTS Disclosed herein is a process for preparing a monoacyl of the formula Image 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 acyl- aldehydes, 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.

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