简多醇及其简化类似物的全合成及抗锥虫活性。
Total Synthesis and Antitrypanosomal Activity of Janadolide and Simplified Analogues.
机构信息
School of Chemistry, The University of Sydney, Sydney, New South Wales 2006, Australia.
Swiss Tropical and Public Health Institute, Socinstrasse 57, 4051 Basel, Switzerland.
出版信息
Org Lett. 2020 Apr 17;22(8):3089-3093. doi: 10.1021/acs.orglett.0c00840. Epub 2020 Apr 6.
Janadolide is a cyclic depsipeptide natural product isolated from the marine cyanobacterium . Herein, we describe the total synthesis of janadolide, along with eight simplified analogues, via an efficient solid-phase strategy. Crucial to the synthesis of the natural product was the construction of a key polyketide fragment via an enantioselective (-)--chlorodiisopinocampheylborane-mediated reduction and a alkyl Suzuki reaction. Janadolide and the simplified analogues exhibited antitrypanosomal activity against pathogenic and parasites.
简多醇是一种从海洋蓝细菌中分离得到的环二肽天然产物。本文通过高效的固相策略，对简多醇及其 8 种简化类似物进行了全合成，并对其进行了描述。该天然产物合成的关键是通过对映选择性（-）--氯代二异松蒎基硼烷介导的还原和烷基 Suzuki 反应构建关键聚酮片段。简多醇及其简化类似物对致病性 和 寄生虫具有抗变形虫活性。
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