期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 3, 页码 728-732出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201608207
关键词
decarboxylation; macrocycles; Michael addition; peptides; photoredox catalysis
资金
- NIH General Medical Sciences (Grant NIHGMS) [R01 GM078201-05]
- Bristol-Myers Squibb
- Merck
- Abbvie
A method for the decarboxylative macrocyclization of peptides bearing N-terminal Michael acceptors has been developed. This synthetic method enables the efficient synthesis of cyclic peptides containing gamma-amino acids and is tolerant of functionalities present in both natural and non-proteinogenic amino acids. Linear precursors ranging from 3 to 15 amino acids cyclize effectively under this photoredox method. To demonstrate the preparative utility of this method in the context of bioactive molecules, we synthesized COR-005, a somatostatin analogue that is currently in clinical trials.
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