Solution-phase automated synthesis of tripeptide derivatives

被引：4

作者：

Kuroda, N

Hattori, T

Kitada, C

Sugawara, T

机构：

[1] Takeda Chem Ind Ltd, Discovery Res Div, Discovery Res Labs 5, Yodogawa Ku, Osaka 5328686, Japan

[2] Takeda Chem Ind Ltd, Div Discovery Res, Tsuchiura, Ibaraki 3004293, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2001年 / 49卷 / 09期

关键词：

automated synthesis; solution-phase peptide synthesis; fragment tripeptide; methanesulfonic acid method; trifluoroacetic acid method;

D O I：

10.1248/cpb.49.1138

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An improved general method for automated synthesis of tripeptides was developed, in which methanesulfonic acid (MSA) was used in place of trifluoroacetic acid (TFA), thus making it possible to avoid, 1) corrosion of the apparatus by strong acid vapor, 2) formation of emulsions, and 3) use of the restricted solvent, dichloromethane. As an application of the automated synthesis apparatus, 216 fragment tripeptide derivatives were synthesized systematically using the MSA method, in excellent yield and with increased efficiency.

引用

页码：1138 / 1146

页数：9

共 23 条

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