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Chemoenzymatic Synthesis of Spinosyn A
Authors:Prof?Dr Hak Joong Kim  Dr Sei‐hyun Choi  Byung‐sun Jeon  Dr Namho Kim  Prof?Dr Rongson Pongdee  Dr Qingquan Wu  Prof?Dr Hung‐wen Liu
Affiliation:1. Division of Medicinal Chemistry, College of Pharmacy and Department of Chemistry, University of Texas at Austin, Austin, TX 78712 (USA);2. Department of Chemistry, Korea University (Republic of Korea);3. Current address: Department of Chemistry, Sewanee: The University of the South (USA)
Abstract:Following the biosynthesis of polyketide backbones by polyketide synthases (PKSs), post‐PKS modifications result in a significantly elevated level of structural complexity that renders the chemical synthesis of these natural products challenging. We report herein a total synthesis of the widely used polyketide insecticide spinosyn A by exploiting the prowess of both chemical and enzymatic methods. As more polyketide biosynthetic pathways are characterized, this chemoenzymatic approach is expected to become readily adaptable to streamlining the synthesis of other complex polyketides with more elaborate post‐PKS modifications.
Keywords:biosynthesis  polyketide macrolides  post‐polyketide synthase modifications  spinosyns  total synthesis
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