Malonate-claisen rearrangement for preparation of integrin receptor antagonist intermediates

摘要

A novel process is provided for the preparation of chiral unsaturated ester intermediates useful in the asymmetric syntheses of α νβ 3 integrin receptor antagonists. The instant process involves an efficient Claisen rearrangement of a malonate ester of a chiral allylic alcohol precursor followed by hydrolysis and decarboxylation. The unsaturated ester intermediates can be converted in a 2-step sequence into the desired substituted nonanoic acid derivatives.