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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.
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页码:6747 / +
页数:8
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