New hypotensive peptides, their preparation and their use
申请人:SANKYO COMPANY LIMITED
公开号:EP0128762A2
公开(公告)日:1984-12-19
Oligopeptides of formula (I)
(wherein R1 CO- is an acyl group, But is an isobutyl or sec-butyl group and X is a variety of organic groups) and salts and esters thereof have valuable renin inhibitory activity and are prepared by conventional polypeptide synthesis.
reaction of 1-(N-acylamino)alkyltriphenylphosphonium tetrafluoroborates with silyl enolates was developed to prepare β-amino carbonyl compounds. The reported method is a useful approach for the preparation of N-protected β-amino esters as well as N-protected β-amino ketones. The starting 1-(N-acylamino)alkyltriphenylphosphonium tetrafluoroborates are readily available from N-protected α-amino acids. Therefore