Gram-scale preparation of the antibiotic lead compound salicyl-AMS, a potent inhibitor of bacterial salicylate adenylation enzymes.
作者： Nihar Kinarivala , Lisa C. Standke , Tezcan Guney , Cheng Ji , Naoyoshi Noguchi
DOI: 10.1016/BS.MIE.2020.04.051
关键词:
摘要: Salicyl-AMS (1) is a potent inhibitor of salicylate adenylation enzymes used in bacterial siderophore biosynthesis and promising lead compound for the treatment tuberculosis. An optimized, multigram synthesis presented, which provides salicyl-AMS as its sodium salt (1·Na) three synthetic steps followed by two-step formation process. The proceeds 11.6% overall yield from commercially available adenosine 2',3'-acetonide highly purified material.
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