Diastereoselective synthesis hydroxyethylene dipeptide isosteres

Details Diastereoselective synthesis hydroxyethylene dipeptide isosteres Diastereoselective synthesis hydroxyethylene dipeptide isosteres

1996-12-24

1999-11-23

O'Sullivan, Peter

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

2609982, 530331, 549321, 560 29, 560 40, 560 43, 560 45, 560125, 560170, 562444, 562445, 562507, 562567, 564134, 564165, 564191, 564197, C07C21922, C07C21906

Patent

active

059903414

ABSTRACT:
A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.

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