Hoshinoamides A, B and C, linear lipopeptides, were isolated from the marine cyanobacterium Caldora penicillata, with potent antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum. Herein, we describe the first total synthesis of Hoshinoamides A. Our synthetic strategy uses the combined methods of solution and solid phase peptide synthesis. Liquid phase synthesis is to improve the coupling yield of L-Val3 and N-Me-D-Phe2. Connecting other amino acids efficiency and convergence by solid state synthesis. This synthetic strategy has good purity and high yield.
Keywords: highly methylated polypeptides; Hoshinoamides; total synthesis; antimalarial
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Zhou, H.; Rui, Z.; Yang, Y.; Xu, S.; Shao, Y.; Liu, L. Beilstein Arch. 2021, 202164. doi:10.3762/bxiv.2021.64.v1
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