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1. 发明授权

US06608208B1 Process for the preparation of 1,2-benzisothiazolin-3-ones 有权
标题翻译： 1,2-苯并异噻唑啉-3-酮的制备方法
公开(公告)号：US06608208B1
公开(公告)日：2003-08-19
申请号：US09298923
申请日：1999-04-26
申请人： Mark Robert James
发明人： Mark Robert James
IPC分类号： C07D27504
CPC分类号： C07D275/04
摘要： A process for making a 2-alkylbenzisothiazolinone which comprises reacting a bisamide of formula in water or an organic liquid containing water with a bisulphite or bisulphite release agent to form a Bunte salt and converting the Bunte salt under alkaline conditions to 2-alkyl-BIT. R is alkyl. Preferred substituents R are butyl, hexyl, 2-ethylbutyl and 2-ethylhexyl.
摘要翻译：一种制备2-烷基苯并异噻唑啉酮的方法，其包括使形式的水的二酰胺或含有水的有机液体与亚硫酸氢盐或亚硫酸氢盐脱模剂反应以形成Bunte盐，并将Bunte盐在碱性条件下转化为2-烷基-BIT。 R是烷基。优选的取代基R是丁基，己基，2-乙基丁基和2-乙基己基。

2. 发明授权

US06562979B1 Process for the preparation of substituted benzisothiazole compounds 失效
标题翻译：取代的苯并异噻唑化合物的制备方法
公开(公告)号：US06562979B1
公开(公告)日：2003-05-13
申请号：US10019466
申请日：2002-07-09
申请人： Gavin David Heffernan
发明人： Gavin David Heffernan
IPC分类号： C07D27504
CPC分类号： C07D275/04 , C07D417/04 , C07D417/14
摘要： A single-step process for the preparation of formula (I) benzisothiazoles from 2-acylphenylthiocyanates. Formula (I) benzisothiazoles are useful as key intermediates in the manufacture of herbicidally active compounds.
摘要翻译：从2-酰基苯基硫氰酸酯制备式（I）苯并异噻唑的单步方法。式（I）苯并异噻唑可用作制造除草活性化合物的关键中间体。

3. 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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