PROCESS FOR PREPARING BENZOXAZIN-4-ONE POLYMER CONJUGATES.

摘要

The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors. The process of the present invention comprises the steps of:a) reacting a polymer or copolymer having the formula (1) wherein R is a hydrocarbyl moiety, a polyalkyleneoxy moiety, or a heteroatom comprising hydrocarbyl moiety, said polymer or copolymer having a molecular weight of from about 500 daltons, with phosgene to form a chloroformate having the formula (2); b) combining a substituted or unsubstituted anthranilic acid having the formula (3) wherein each R1 unit is an enzyme interaction attenuating unit; and a base catalyst wherein said base catalyst is a supported base catalyst, to form a substrate reactive admixture; and c) adding to said chloroformate formed in step (a) said substrate reactive admixture formed in step (b) to form a benzoxazin-4-one conjugate having the formula (4).