Patent ID: 8784791
Filing Date: 2014-07-22
Classification: A61K,C07D,C08G,C08L

Abstract:
1. A method for forming an N-succinimidyl ester of a water-soluble polymer from an ortho ester of the water-soluble polymer, the method comprising the steps of: (i) conducting acid-catalyzed hydrolysis of the ortho ester of the water-soluble polymer to provide an intermediate ester of a water-soluble polymer; (ii) conducting base-promoted hydrolysis on the intermediate ester of the water-soluble polymer to provide the water-soluble polymer bearing a terminal carboxylic acid; and (iii) esterifying the water-soluble polymer bearing a terminal carboxylic acid using N-hydroxysuccinimide to form the N-succinimidyl ester of a water-soluble polymer, wherein the ortho ester of the water-soluble polymer has the following structure: the water-soluble polymer bearing a terminal carboxylic has the following structure: and further wherein, for each of these structures, POLY is a water-soluble polymer; (a) is either zero or one; X, when present, is a spacer moiety; (z) is an integer from 1 to 24; R R each R