Daniel R. Sidler

The enantioselective synthesis of LTD4 antagonist L-708,738

Abstract An efficient, 9-step synthesis of LTD 4 antagonist L-708,738 is described. The asymmetric center is set via a chiral borane reduction.

Enzymes and practical asymmetric synthesis

A practical, chemoenzymatic, four-step synthesis of the LTD4 antagonist MK-0679 is described. The key steps are enzymatic hydrolysis of the prochiral diester to the ester-acid in 99% enantiomeric excess followed by aluminum mediated amidation of the methyl ester to afford MK-0679 in high overall yield. This synthesis is superior to the synthesis of the racemate MK-0571.