Decarboxylative Peptide Macrocyclization through Photoredox Catalysis.
نویسندگان
چکیده
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 γ-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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عنوان ژورنال:
- Angewandte Chemie
دوره 56 3 شماره
صفحات -
تاریخ انتشار 2017