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1. 发明授权

US06350879B1 Benziso-N (L-histidine methylester)-thiazolone, process for the preparation thereof, and use thereof for RNA polymerase inhibition 有权
标题翻译： Benziso-N（L-组氨酸甲酯） - 噻唑酮，其制备方法及其用于RNA聚合酶抑制的用途
公开(公告)号：US06350879B1
公开(公告)日：2002-02-26
申请号：US09724499
申请日：2000-11-28
申请人： Subramania Ranganathan , Kannoth Manjheri Muraleedharan
发明人： Subramania Ranganathan , Kannoth Manjheri Muraleedharan
IPC分类号： C07D27504
CPC分类号： C07D417/06
摘要： The present invention discloses novel benziso-N(L-histidine methylester)-thiazolone compound of the formula 3 useful as a RNA polymerase inhibitor. These compounds are prepared by generating the free amine of the histidine methylester in situ by the addition of triethylamine to an ice cooled and stirred suspension of histidine methylester dihydrochloride in dry dichloromethane, adding dropwise, a dichloromethane solution of dithiodibenzoyl chloride and triethylamine to the said free amine at a temperature in the range of 0-5° C. to room temperature, stirring the reaction mixture for about 48 h, washing said reaction mixture with cold saturated NaHCO3, subjecting it to a conventional organic-layer drying , followed by evaporating the solvent in vacuo, and eluting by chromatography the residue benziso-N(L-histidine methylester)-thiazolone.
摘要翻译：本发明公开了用作RNA聚合酶抑制剂的式3的新型苯并异-N（L-组氨酸甲酯） - 噻唑酮化合物。这些化合物是通过将三乙胺加入到冷冻和搅拌的组氨酸甲酯二盐酸盐的无水二氯甲烷悬浮液中而立即产生组氨酸甲酯的游离胺而制备的，滴加二硫代二苯甲酰氯和三乙胺的二氯甲烷溶液至所述游离的胺，在0-5℃至室温的温度下搅拌反应混合物约48小时，用冷的饱和NaHCO 3洗涤反应混合物，使其经历常规的有机层干燥，然后蒸发溶剂，并通过色谱法洗脱，得到残余物benziso-N（L-组氨酸甲酯） - 噻唑酮。

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