CAS: 16133-49-6; 5-Methoxy-2-Nitrophenylamine

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📜5-甲氧基-2-硝基苯甲酸置于盐酸,二苯基磷酸,三乙胺体系中,用 甲醇 用作溶剂,化学反应 112.0H,反应生成5-甲氧基-2-硝基苯胺
参考文献:1,2,4-苯并三嗪1,4-二氧化物作为替拉帕明的低氧选择性类似物的构效关系.
标题:1,2,4-苯并三嗪1,4-二氧化物作为替拉帕明的低氧选择性类似物的构效关系.
摘要:替拉帕明(tpz,1,2,4-苯并三嗪-3-胺1,4-二氧化物)是一种生物还原性低氧细胞毒素,目前在ii / Iii期临床试验中结合放疗和基于顺铂的化学疗法.作为开发具有改善的溶解度/效能和治疗指数的tpz类似物的程序的一部分,我们合成了34 1,2,4-苯并三嗪-3-胺1,4-二氧化物(bto),以检查其结构活性关系(sar).环取代.系统地改变了5,6,7和8位上取代基的电子,疏水和空间参数,并确定了类似物的水溶性和单电子还原电位[e(1)] .对于每种化合物,我们通过克隆形成存活率确定了有氧和低氧条件下小鼠sccvii肿瘤细胞的体外杀伤作用,并确定了它们的相对低氧毒性(rht;相对于tpz)和低氧细胞毒性比(hcr).使用96孔srb增殖测定法独立评估了化合物的子集,其数据与克隆形成终点所得出的数据具有非常好的相关性.除5-和8-二甲基氨基和8-二乙基氨基外,大多数取代基的溶解度均低于tpz.E(1)值的范围是-240
Doi:10.1021/jm020367+

专利信息

专利号:US-6753347-B2
优先权日:1999-06-28
标题:Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof
发明人：KISHI NAOYUKI; NAKAMURA YOSHITAKA; ABE NARUMI; TAKEBAYASHI TOYONORI
权利人:SANKYO CO
摘要:This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, n wherein R 1 is C 1 -C 6 alkyl, C 1 -C 6 alkoxyl, etc., R 2 is C 1 -C 6 alkyl, and R 3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.

专利号:US-2003199580-A1
优先权日:1999-06-28
标 题:Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof

专利号:US-6525220-B2
优先权日:1999-06-28
标 题 :Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof

专利号:EP-1191019-B1
优先权日:1999-06-28
标题:Intermediates for the synthesis of benzimidazole compounds and process for the preparation thereof

专利号:EP-1191019-A1
优先权日:1999-06-28
标题 :Intermediates for the synthesis of benzimidazole compounds and process for the preparation thereof

专利号:US-2003008907-A1
优先权日:1999-06-28
标 题:Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof