期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 139, 期 20, 页码 6815-6818出版社
AMER CHEMICAL SOC
DOI: 10.1021/jacs.7b02515
关键词
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资金
- National Young 1000 Talents Plan Program
- College of Chemistry and Molecular Engineering, Peking University
- Peking-Tsinghua Center for Life Sciences
- National Science Foundation of China [21472003, 31521004, 21672011]
A concise and enantioselective total synthesis of the potent PI3K inhibitor (+)-wortmannin is described. A Pd-catalyzed cascade reaction was first developed to connect a synthon derived from Hajos Parrish ketone to a furan moiety. The subsequent Friedel Crafts alkylation of the beta-position of a furan ring to an epoxide was optimized to establish the C10 quaternary center. (+)-Wortmannin was eventually accomplished by transformations following a late-stage oxidation of the furan allylic position. Kinome profiling and in vitro enzymatic assays were performed on 17-beta-hydroxy-wortmannin and an epoxide analogue.
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