Solid-phase total synthesis of polymyxin B1

被引:27
作者
Sharma, SK [1 ]
Wu, AD [1 ]
Chandramouli, N [1 ]
Fotsch, C [1 ]
Kardash, G [1 ]
Bair, KW [1 ]
机构
[1] Novartis Inst Biomed Res, Dept Oncol, Summit, NJ 07901 USA
来源
JOURNAL OF PEPTIDE RESEARCH | 1999年 / 53卷 / 05期
关键词
Fmoc-Dab(Dde); polymyxin B1; S-(+)-6-methyloctane-1-carboxylic acid; solid-phase synthesis;
D O I
10.1034/j.1399-3011.1999.00045.x
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The total solid-phase synthesis of polymyxin B1 (PMB1) has been achieved in 20% yield using the orthogonal protecting group N-1-(4,4-dimethyl-2,6-dioxocyclohexylidene)ethyl-(Dde). This report demonstrates that a complex peptide macrocycle can be synthesized in high yields using solid-phase synthesis. According to MS and HPLC, the synthetic peptide was identical to the naturally occurring antibiotic.
引用
收藏
页码:501 / 506
页数:6
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