2-mercaptopyridine-1-oxide-based peptide coupling reagents

被引:23
作者
Albericio, F
Bailén, MA
Chinchilla, R
Dodsworth, DJ
Nájera, C
机构
[1] Univ Alicante, Fac Ciencias, Dept Quim Organ, E-03080 Alicante, Spain
[2] Univ Barcelona, Dept Quim Organ, E-08028 Barcelona, Spain
关键词
thiouronium; ureas; coupling reagents; peptides; solid-phase;
D O I
10.1016/S0040-4020(01)00985-1
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The thiouronium salts S-(1-oxido-2-pyridinyl)-1,1,3,3-tetramethylthiouronium hexafluorophosphate (HOTT) and tetrafluoroborate (TOTT), and S-(1-oxido-2-pyridinyl)-1,3-dimethyl-1,3-trimethylenethiouronium hexafluorophosphate (HODT) and tetrafluoroborate (TODT), prepared from 2-mercaptopyridine-1-oxide and 1, 1,3,3-tetramethylurea (TMU) or 1,3-dimethylpropyleneurea (DMPU), have been employed as reagents in solution and solid-phase peptide coupling chemistry. Furthermore, 2-mercaptopyridine-1-oxide has been employed as racemization-reducing additive combined with the new thiouronium salts and other frequently used peptide coupling reagents such as DCC or TBTU. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:9607 / 9613
页数:7
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