Patent ID: 6180759
Filing Date: 2001-01-30
Classification: A61P,C07D,C07K,Y02P

Abstract:
A process for preparing a pseudotetrapeptide compound of formula ##STR51##or a salt or prodrug thereof wherein ##STR52##is optionally nitrogen protected azaheterocyclyl; ##STR53##is a single or double bond;q is 1-5;B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl;Q.sub.2 is H or a carboxylic acid protecting group;J is --H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl or substituted aralkyl;L is OR.sup.1, or NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are independently --H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; andp is 1 or 2, comprising(a) coupling an azaheterocyclyl pseudodipeptide of formula ##STR54##or a salt thereof wherein K is OH or an acyl activating group, with a carboxylic acid substituted dipeptide of formula ##STR55##or a salt thereof,(b) optional removing the nitrogen protecting group or carboxylic acid protecting group and(c) optionally converting the pseudotetrapeptide to the salt or prodrug.