Process for producing peptide derivatives and salts therefor

Details Process for producing peptide derivatives and salts therefor Process for producing peptide derivatives and salts therefor

1994-12-28

1997-07-01

Russel, Jeffrey E.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Tripeptides, e.g., tripeptide thyroliberin , etc.

530332, 530337, 530338, 530340, 530341, C07K 102, C07K 108, C07K 110, C07K 5083

Patent

active

056440286

ABSTRACT:
A process for producing peptide derivatives of formula (1) or salts thereof: ##STR1## which comprises condensation of peptide derivative of formula (2): ##STR2## with carboxylic acid of formula (3): ##STR3## or condensation of a peptide derivative of formula (4): ##STR4## with a protected amino acid of formula (5'): ##STR5## wherein R.sup.1 and R.sup.2 are a lower alkyl group or hydrogen atom, R.sup.3 is a lower alkyl group, X is a methylthiomethyl, methanesulfonylmethyl, carbamoylmethyl, or a lower alkyl group, Ar is an aryl or heteroaryl group, and A.sup.4 is Ar--O--CH.sub.2 --CO. The peptide derivatives and salts thereof are useful as the human immunodeficiency virus (HIV) protease inhibitors.

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T. Mimoto et al., 117:8449h "Design and synthesis of HIV protease inhibitors containing a hydroxmethylcarbonyl isostere as a transition-state mimic", Chemical Abstracts, 117(1):2(1992).

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