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
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
收藏
页码:6931 / 6935
页数:5
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