Hydantoin intermediates for the synthesis of omapatrilat and methods for producing and using the same

摘要

Omapatrilat (I) is a potent inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) both in vitro and in vivo and is currently undergoing large scale clinical trials as an anti-hypertensive. Omapatrilat may be synthesized using the S-stereoisomer of compound (V). Compound (V) may be prepared from a novel hydantoin (III). The hydantoin may be prepared from a monoacetal (XI) or via a dinitrile (V).