CAS: 50820-65-0; Methyl 1H-Indole-6-Carboxylate

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4-甲基-3-硝基苯甲酸置于palladium On Activated Charcoal 盐酸,氢气体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 14.5H,反应生成 吲哚-6-甲酸甲酯
参考文献:Thromboxane A2 Synthetase Inhibitors With Histamine H1-Blocking Activity: Synthesis And Evaluation Of A New Series Of Indole Derivatives.
标题:Thromboxane A2 Synthetase Inhibitors With Histamine H1-Blocking Activity: Synthesis And Evaluation Of A New Series Of Indole Derivatives.
摘要:制备了一系列n-取代的3-(1H-咪唑-1-基甲基)吲哚羧酸衍生物,并评估了它们对血栓素a2(txa2)合成酶抑制和组胺h1受体阻断的活性.在合成的化合物中,6-吲哚羧酸衍生物显示出比其他位置异构体更高的活性.1-[3-(4-苯并氢吡啶-1-基)丙基]-3-(1H-咪唑-1-基甲基)-1H-吲哚-6-羧酸(12)具有最强的血栓素合成酶抑制活性(ic50=5x10-8M)和h1受体阻断活性(ic50=8x10-9M).
DOI:10.1248/cpb.43.1692

专利信息

专利号:US-4841045-A
优先权日:1985-03-12
标 题 :Synthesis of vinblastine and vincristine type compounds
发明人：KUEHNE MARTIN
权利人:UNIV VERMONT
摘要:A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.

专利号:US-4897477-A
优先权日:1985-03-12
标题:Synthesis of vinblastine and vincristine type compounds
发明人：KUEHNE MARTIN
权利人:UNIV VERMONT
摘要:A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.

专利号:WO-8605491-A1
优先权日:1985-03-12
标 题 :Synthesis of vinblastine and vincristine type compounds

专利号:EP-1957644-B1
优先权日:2005-12-01
标 题 :Enzymatic encoding methods for efficient synthesis of large libraries

专利号:RU-2042666-C1
优先权日:1990-08-15
标题:Method of synthesis of substituted hexahydrobenz[cd]indoles

专利号:EP-0215058-A1
优先权日:1985-03-12
标题:Synthesis of vinblastine and vincristine type compounds