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
收藏
页码：5981 / 5984
页数：4
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