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学科主题: 氟化学
题名: Coupling of sterically hindered aldehyde with fluorinated synthons: Stereoselective synthesis of fluorinated analogues of salinosporamide A
其他题名: 空间位阻醛和含氟合成子的偶联反应: salinosporamide A.的立体选择性合成
作者: Chen ZH(陈增浩) ; Wang BL(王炳林) ; Andrew J. Kale ; Bradley S. Moore ; Wang RW(王若文) ; Qing FL(卿凤翎)
通讯作者: 卿凤翎
刊名: J. Fluor. Chem.
发表日期: 2012
卷: 136, 页:12-19
收录类别: SCI
部门归属: 中科院上海有机化学研究所; 美国加州大学圣地亚哥分校
英文摘要: Salinosporamide A is an irreversible inhibitor of the beta-subunits of the 20S proteasome. Its C-5 cyclohexenyl moiety is the key to its affinity and potency as an anticancer agent. Here we describe the synthesis of C-5 difluoromethylated and trifluoromethylated analogues of salinosporamide A and their biological evaluation as proteasome inhibitors against purified yeast 20S proteasome. The synthetic strategy featured the stereoselective coupling reaction of sterically hindered aldehyde 3 with fluorinated organolithium reagents. (C) 2012 Elsevier B.V. All rights reserved.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000302976900003
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/28263
Appears in Collections:中科院有机氟化学重点实验室_期刊论文

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Recommended Citation:
Chen ZH,Wang BL,Andrew J. Kale,et al. Coupling of sterically hindered aldehyde with fluorinated synthons: Stereoselective synthesis of fluorinated analogues of salinosporamide A[J]. J. Fluor. Chem.,2012,136:12-19.
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