Improved total synthesis of the antibiotic A54145B
Hoi Yee Chow1, Delin Chen1, Xuechen Li1
1Department of Chemistry, State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong, P. R. China. xuechenl@hku.hk.
Organic & Biomolecular Chemistry
|April 17, 2020
Abstract:
A54145B is a calcium-dependent cyclic lipodepsipeptide antibiotic that is active against Gram-positive pathogens. Herein, we report an improved synthetic route toward A54145B in terms of the yield and time required. The key changes include using a pre-assembled minimalist tetradepsipeptide building block to solve the difficult on-resin esterification from our previous synthetic route, and a new macrocyclization site to avoid the peptide self-cleavage problem.
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