School of Chemistry, University of Bristol, Cantock's Close, Bristol BS8 1TS, United Kingdom.
Laboratory of Gene Technology, KU Leuven, Kasteelpark Arenberg 21, P.O. Box 2462, 3001 Leuven, Belgium.
Org Lett. 2020 Aug 21;22(16):6349-6353. doi: 10.1021/acs.orglett.0c02190. Epub 2020 Aug 10.
The kalimantacins make up a family of hybrid polyketide-nonribosomal peptide-derived natural products that display potent and selective antibiotic activity against multidrug resistant strains of . Herein, we report the first total synthesis of kalimantacin A, in which three fragments are prepared and then united via Sonogashira and amide couplings. The enantioselective synthetic approach is convergent, unlocking routes to further kalimantacins and analogues for structure-activity relationship studies and clinical evaluation.
卡利曼他汀是一类由杂合聚酮-非核糖体肽衍生的天然产物组成的家族，对多种耐药菌株具有强大而选择性的抗生素活性。在此，我们首次报道了卡利曼他汀 A 的全合成，其中通过 Sonogashira 和酰胺偶联反应制备了三个片段，然后将它们连接在一起。该对映选择性合成方法具有收敛性，为进一步研究卡利曼他汀及其类似物的结构-活性关系以及临床评估开辟了途径。
