Preparation of active esters on solid support for aqueous-phase peptide couplings

被引:17
作者
Corbett, AD [1 ]
Gleason, JL [1 ]
机构
[1] McGill Univ, Dept Chem, Montreal, PQ H3A 2K6, Canada
关键词
D O I
10.1016/S0040-4039(01)02389-9
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
TentaGel supported active esters analogous to those prepared from solution-phase 1-hydroxybenzotriazole. N-hydroxysuccinimide and pentafluorophenol were prepared and examined for their ability to effect aqueous-phase peptide couplings. HOBt esters showed high hydrolysis rates, relative to peptide coupling. while active esters derived from 4-hydroxy-2.3.5.6-tetrafluorobenzoic acid produced mainly dipeptide coupling products when treated with amino acids in water. (C) 2002 Elsevier Science Ltd. All rights reserved.
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页码:1369 / 1372
页数:4
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