Process for the preparation of intermediates for the manufacture of NEP inhibitors

摘要

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

主权项

1. A process for preparing a compound of formula (3), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, such as BOC; and R3 is a carboxyl group or an ester group, preferably a carboxyl group, said process comprising reacting a compound of formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group; and R3 is a carboxyl group or an ester group, preferably a carboxyl group; with a transition metal catalyst, optionally in the presence of a base, to obtain the compound of formula (3), or salt thereof.