大环二氧杂环戊酮 A 的全合成。
Total Synthesis of Macrocyclic Dysoxylactam A.
机构信息
Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, 1200 Cai Lun Road, Shanghai, 201203, China.
State Key Laboratory of Bio-organic and Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.
出版信息
Chem Asian J. 2020 Aug 17;15(16):2467-2469. doi: 10.1002/asia.202000482. Epub 2020 Jul 15.
The total synthesis of dysoxylactam A, a novel 17-membered macrolactam with potent multi-drug-resistant reversing activities, has been achieved, starting from 4-pentene-1-al in a longest linear sequence of 17 steps and 9.5% overall yield. The key transformations consist of iterative aldol and ring-closing metathesis reactions for the construction of the stereochemically enriched polypropionate scaffold and the macrocycle, respectively.
多西拉米胺 A 的全合成，一种新型的 17 元大环内酯，具有很强的多药耐药逆转活性，已经实现，从 4-戊烯-1-醛开始，最长线性序列为 17 步，总收率为 9.5%。关键转化包括迭代醛缩合和环 closing metathesis 反应，分别用于构建立体化学丰富的聚丙酸盐支架和大环。
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