A Total Synthesis of Salinosporamide A

被引:23
|
作者
Marx, Leo B. [1 ]
Burton, Jonathan W. [1 ]
机构
[1] Univ Oxford, Dept Chem, Chem Res Lab, Mansfield Rd, Oxford OX1 3TA, England
基金
英国工程与自然科学研究理事会;
关键词
cyclization; natural products; proteasome inhibitor; radicals; total synthesis; CARBOXYLIC-ACID DERIVATIVES; FREE-RADICAL CYCLIZATION; CONCISE TOTAL-SYNTHESIS; FORMAL SYNTHESIS; ASYMMETRIC ALKYLATION; PROTEASOME INHIBITORS; BETA-LACTAMS; (-)-SALINOSPORAMIDE; ANALOGS; ROUTE;
D O I
10.1002/chem.201800046
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Salinosporamide A is a beta-lactone proteasome inhibitor currently in clinical trials for the treatment of multiple-myeloma. Herein we report a short synthesis of this small, highly functionalized, biologically important natural product that uses an oxidative radical cyclization as a key step and allows for the preparation of gram quantities of advanced synthetic intermediates.
引用
收藏
页码:6747 / +
页数:8
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