OXYBENZOTRIAZOLE FREE PEPTIDE COUPLING REAGENTS FOR N-METHYLATED AMINO-ACIDS

被引：170

作者：

COSTE, J ^{[1
]}

FREROT, E ^{[1
]}

JOUIN, P ^{[1
]}

CASTRO, B ^{[1
]}

机构：

[1] SANOFI CHIM,F-75008 PARIS,FRANCE

来源：

TETRAHEDRON LETTERS | 1991年 / 32卷 / 17期

关键词：

PEPTIDE; COUPLING REAGENT; N-METHYL AMINO ACID; HYDROXYBENZOTRIAZOLE;

D O I：

10.1016/0040-4039(91)85015-W

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The main product of N-methylated amino acid coupling, when oxybenzotriazole is present in the reagent (BOP, PyBOP, HBPyU) or as an additive (DCC/HOBt), is the weakly reactive benzotriazolyl ester. On the other hand, the corresponding new halogenated reagents PyBroP, PyCloP and PyClU give very good results and can be recommended.

引用

页码：1967 / 1970

页数：4

共 17 条

[1]

CASTRO B, 1975, TETRAHEDRON LETT, P1219

[2]

CASTRO B, 1973, TETRAHEDRON LETT, P3243

[3] N-METHYLAMINO ACIDS IN PEPTIDE-SYNTHESIS .6. METHOD FOR DETERMINING ENANTIOMERIC PURITY OF N-METHYLAMINO ACIDS AND THEIR DERIVATIVES BY ION-EXCHANGE CHROMATOGRAPHY AS THEIR C-TERMINAL LYSYL DIPEPTIDES [J].