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Enzymatic Synthesis of a CCK-8 Tripeptide Derivative
作者姓名:Li  GUO  Zi  Min  LU
作者单位:Li GUO1*,Zi Min LU2,Heiner ECKSTEIN3 1West China School of Pharmacy,Sichuan University,Chengdu 610041 2Tongji Medical College,Huazhong Science & Technology University,Wuhan 430030 3Institute of Organic Chemistry,University of Tuebingen,72076 Tuebingen,Germany
摘    要:The enzymatic synthesis of CCK-8 tripeptide derivative Phae-Met-Asp(OMe)-Phe-NH2 is reported.Starting with Phac-Met-OCam,we have successfully synthesized the target tripeptide with three free or immobilized enzymes, α-chymotrypsin,papain and thermolysin in reasonable yields.The key steps in this synthesis were the coupling of Phac-Met-OCam and H-Asp(OMe)2 to from Met-Asp peptide bond catalyzed by α-chymotrypsin and the selective hydrolysis of α-ester of Phac-met-Asp(OMe)2 catalyzed by papain.

关 键 词:CCK-8  三肽衍生物  选择性合成  木瓜蛋白酶  酶催化合成

Enzymatic Synthesis of a CCK-8 Tripeptide Derivative
Li GUO,Zi Min LU,Heiner Eckstein.Enzymatic Synthesis of a CCK-8 Tripeptide Derivative[J].Chinese Chemical Letters,2003,14(2):167-168.
Authors:Li GUO  Zi Min LU  Heiner Eckstein
Abstract:The enzymatic synthesis of CCK-8 tripeptide derivative Phac-Met-Asp(OMe)-Phe-NH2 is reported. Starting with Phac-Met-OCam, we have successfully synthesized the target tripeptide with three free or immobilized enzymes, ?chymotrypsin, papain and thermolysin in reasonable yields. The key steps in this synthesis were the coupling of Phac-Met-OCam and H-Asp(OMe)2 to form Met-Asp peptide bond catalyzed by ?chymotrypsin and the selective hydrolysis of -ester of Phac-Met-Asp(OMe)2 catalyzed by papain.
Keywords:Enzymatic synthesis  CCK-8  tripeptide derivative  
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