Effects of amounts of additives on peptide coupling mediated by a water-soluble carbodiimide in alcohols

被引：17

作者：

Nozaki, S ^{[1
]}

机构：

[1] Josai Univ, Fac Pharmaceut Sci, Sakado, Saitama 3500295, Japan

来源：

JOURNAL OF PEPTIDE RESEARCH | 1999年 / 54卷 / 02期

关键词：

alcoholic solvent; ester formation; HOBt; HOOBt; HOAt; peptide synthesis; water-soluble carbodiimide;

D O I：

10.1034/j.1399-3011.1999.00101.x

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The optimal amounts of 1-hydroxybenzotriazole (HOBt), 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine (HOOBt) and 1-hydroxy-7-azabenzotriazole (HOAt) for enhancement of peptide coupling mediated by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) hydrochloride in alcoholic solvents were found to be less than equimolar against the carboxyl component or the carbodiimide. In comparison with the use of equimolar additives, the use of less equimolar ones was more effective in suppressing the competitive ester formation and in increasing the yield of desired peptides. EDC hydrochloride/around 0.1 equimolar HOAt or HOOBt were efficient reagents for peptide synthesis in the media.

引用

页码：162 / 167

页数：6

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