ANGIOTENSIN I - CONVERTING ENZYME (ACE) INHIBITORS

摘要

This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro ("keto-ACE", compound 5a) and analogues thereof. The synthesis process proceeds via an .alpha.,~-unsaturat ed keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the , -unsaturated keto-phoshonate with ethyl gyloxylate. Ket o- ACE analogues produced by the process of the invention display C-domain selectivity.