期刊
ORGANIC LETTERS
卷 -, 期 -, 页码 -出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.2c02870
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资金
- KAKENHI
- Japan Society for the Promotion of Science
- [JP20K15407]
- [JP16H06444]
- [JP20H05618]
- [JP19K22243]
- [JP20H02866]
This article presents a strategy for synthesizing novel lactazole-like thiopeptides, including the preparation of central triheterocyclic amino acid and its use in solid-phase peptide synthesis, as well as a technique for preparing C-terminally functionalized thiopeptides for biological studies. The synthesis of 11 TNIK-inhibitor thiopeptides and 6 derivatives highlights the practicality of the developed protocols.
A strategy for the synthesis of de novo discovered lactazole-like thiopeptides is reported. The approach revolves around a convergent and scalable preparation of the central triheterocyclic amino acid and its utilization in Fmoc solid-phase peptide synthesis for modular peptide chain assembly. A technique for preparing C-terminally functionalized thiopeptides for biological studies is also described. The syntheses of 11 TNIK-inhibitor thiopeptides and 6 of their derivatives in multimilligram quantities highlight the practical utility of the developed protocols.
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