Rapid microwave-assisted solution-phase peptide synthesis

被引：34

作者：

Mahindra, Amit ^{[1
]}

Sharma, Krishna K. ^{[1
]}

Jain, Rahul ^{[1
]}

机构：

[1] Natl Inst Pharmaceut Educ & Res, Dept Med Chem, Sas Nagar 160062, Punjab, India

来源：

TETRAHEDRON LETTERS | 2012年 / 53卷 / 51期

关键词：

Solution-phase peptide synthesis; Microwave-assisted synthesis; Activators; Boc chemistry; Fmoc chemistry; SPEED SOLUTION SYNTHESIS; AMINO-ACID; ORGANIC-SYNTHESIS; IN-VITRO; ANTIMICROBIAL PEPTIDES; ANTIFUNGAL PEPTIDE; RICH PEPTIDES; IRRADIATION; SEQUENCES; ARGININE;

D O I：

10.1016/j.tetlet.2012.10.028

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Rapid microwave-assisted solution-phase peptide synthesis protocol has been developed. The reaction temperature of 50 degrees C. 40 W and short coupling time of 28 min gave racemization-free synthesis of peptides in 50-80% yield. The method is applicable with equal ease in coupling both side-chain protected and unprotected amino acids indicating reactive-functional group tolerance and high atom-economy. In the case of dipeptides, DIC/HONB-mediated coupling rendered the best results. In the case of tri- and tetrapeptides, HATU/HOAt/DIEA emerged as the best coupling combination. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：6931 / 6935

页数：5

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