Process and intermediates for making substituted aspartic acid acetals

摘要

Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: wherein R¹ is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R² is preferably a P₂-P₄ moiety of a caspase inhibitor. Key intermediates include the azidolactones III and VIII: