希玛他汀的全合成。
Total synthesis of himastatin.
机构信息
Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
The Koch Institute for Integrative Cancer Research, MIT, Cambridge, MA 02142, USA.
出版信息
Science. 2022 Feb 25;375(6583):894-899. doi: 10.1126/science.abm6509. Epub 2022 Feb 24.
Abstract
The natural product himastatin has an unusual homodimeric structure that presents a substantial synthetic challenge. We report the concise total synthesis of himastatin from readily accessible precursors, incorporating a final-stage dimerization strategy that was inspired by a detailed consideration of the compound's biogenesis. Combining this approach with a modular synthesis enabled expedient access to more than a dozen designed derivatives of himastatin, including synthetic probes that provide insight into its antibiotic activity.
摘要
天然产物海兔素具有不寻常的同源二聚体结构，这给其合成带来了巨大的挑战。我们报道了海兔素的简洁全合成，该合成从易得的前体出发，采用最终阶段的二聚化策略，该策略受到了对该化合物生物合成的详细考虑的启发。将这种方法与模块化合成相结合，使我们能够快速获得十几种设计的海兔素衍生物，包括提供其抗生素活性见解的合成探针。
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