COMPARATIVE-STUDIES OF THE COUPLING OF N-METHYLATED, STERICALLY HINDERED AMINO-ACIDS DURING SOLID-PHASE PEPTIDE-SYNTHESIS

被引：69

作者：

ANGELL, YM

GARCIAECHEVERRIA, C

RICH, DH

机构：

[1] UNIV WISCONSIN,DEPT CHEM,MADISON,WI 53706

[2] UNIV WISCONSIN,SCH PHARM,MADISON,WI 53706

来源：

TETRAHEDRON LETTERS | 1994年 / 35卷 / 33期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/0040-4039(94)88054-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Comparison of different coupling reagents for effective coupling of N-methylated, sterically hindered amino acids under solid-phase peptide synthesis (SPPS) conditions is described. Superior results were obtained with the coupling additive 1-hydroxy-7-azabenzotriazole (HOAt), as well as its uronium salt derivative (HATU), which both produced quantitative couplings. Application of these regents to the synthesis of the 2-7 sequence found in cyclosporin is reported.

引用

页码：5981 / 5984

页数：4

共 28 条

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