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学科主题: 有机化学
题名: General and stereospecific route to 9-substituted, 8,9-disubstituted, and 9,10-disubstituted analogues of benzolactm-V8
其他题名: 一个通用和立体专一性的途径来合成9-取代8,9-二取代9,10-二取代的苯并八元内酰胺类似物
作者: Ma DW(马大为) ; Tang WJ(汤文军) ; Kozikowski*, Alan P ; Lewin, Nancy E. ; Blumberg Peter M.
通讯作者: 马大为 ; Kozikowski*, Alan P
刊名: J. Org. Chem.
发表日期: 1999-01-01
卷: 64, 页:6366-6373 J. Org. Chem. 1999, 64, 6366-6373
收录类别: SCI
部门归属: 中国科学院上海有机化学研究所生命有机化学国家重点实验室; Georgetown University Medical Center, National Cancer Institute Bethesda, Maryland
英文摘要: Nitration of the L-tyrosine derivative 9 provides the 3-nitro compound 13, which is converted into amide 15 by reduction and protection. Nitration of 15 either ortho or para to the acetamido group gives 16 and 17. After reduction of the nitro group, the anilines 21b and 29b are coupled with triflate 22a, and then cyclized to afford lactams 24 and 31, respectively. By means of a Pd-catalyzed coupling reaction, 8-acetamido-9-decynylbenzolacam-V8(33) are obtained. The regiosiomers 16 and 17 are transformed into a single isomer, 34, which is converted into 9-decynylbenzolactam-V8 (4). The Ki values for 4, 26, and 33 to displace PDBU binding from recombinant PKCα(PKC=protein kinase C) are about 6, 173, and 46 nM. These results demonstrate that while the introduction of a substitutent at either the 8-or 10-position of the 9-substituted benzolactam-V8s lowers their binding affinity, these newly generated analogues still retain reasonably good potency for PKC.
语种: 英语
相关网址: 查看原文
内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/15341
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
Ma DW,Tang WJ,Kozikowski*, Alan P,et al. General and stereospecific route to 9-substituted, 8,9-disubstituted, and 9,10-disubstituted analogues of benzolactm-V8[J]. J. Org. Chem.,1999,64:6366-6373 J. Org. Chem. 1999, 64, 6366-6373.
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