title: Chemo-enzymatic synthesis of tripeptide RGD diamide in organic solvents.
abstract: The tripeptide BzArgGlyAsp(NH(2))(2) was synthesized by a combination of chemical and enzymatic methods in this study. First of all, GlyAsp(NH(2))(2) was synthesized by a novel chemical method in three steps including chloroacetylation of L-aspartic acid, esterification of chloroacetyl L-aspartic acid and ammonolysis of chloroacetyl L-aspartic acid diethyl ester. Secondly, kinetically controlled synthesis of BzArgGlyAsp(NH(2))(2) catalyzed by trypsin in organic solvent was conducted. The optimum conditions are pH 8.0, 30 degrees C in ethanol/Tris-HCl buffer system (85:15, v/v) for 80 min in the maximum yield of 74.4%.
authors.affiliation: Key Laboratory for Molecular Enzymology and Engineering of Ministry of Education, Jilin University, Changchun 130023, PR China.
authors.forename: Yi-Bing
authors.initials: YB
authors.lastname: Huang
authors.forename: Yu-Peng
authors.initials: YP
authors.lastname: Xiao
authors.forename: Hua
authors.initials: H
authors.lastname: Wang
authors.forename: Rui-Zhen
authors.initials: RZ
authors.lastname: Hou
authors.forename: Na
authors.initials: N
authors.lastname: Zhang
authors.forename: Xiao-Xia
authors.initials: XX
authors.lastname: Wu
authors.forename: Li
authors.initials: L
authors.lastname: Xu
authors.forename: Xue-Zhong
authors.initials: XZ
authors.lastname: Zhang
mesh_terms: D000577:Amides / Q000737:chemistry*; D004951:Esterification; D009842:Oligopeptides / Q000737:chemistry*; D009930:Organic Chemicals / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry*
chemical_list: D000577:Amides; D009842:Oligopeptides; D009930:Organic Chemicals; D012997:Solvents; C047981:arginyl-glycyl-aspartic acid