首页> 外国专利> A PROCESS FOR MAKING THE CRYSTAL FORM I OF 4-{5-(4-FLUOROPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL-BENZENESULFONAMIDE

A PROCESS FOR MAKING THE CRYSTAL FORM I OF 4-{5-(4-FLUOROPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL-BENZENESULFONAMIDE

机译:制备4- {5-(4-氟苯基)-3-(三氟甲基)-1H-吡唑-1-基]-苯磺酰胺晶体形式I的方法

摘要

(a) mixing 1.0 to 1.6 moles of alkyl trifluoroacetate per mole of 4-fluoroacetophenone, 1.0 to 1.5 moles of a metal alkoxide per mole of 4-fluoroacetophenone, and a known quantity of 4-fluoroacetophenone to make a mixture; (b) combining the mixture from step (a) with a combination of 415 to 1,245 ml of water per mole of 4-fluoroacetophenone, 1.1 to 2.0 moles of concentrated hydrochloric acid per mole of 4-fluoroacetophenone, 0.8 to 1.2 moles of 4-sulfonamidophenylhydrazine hydrochloride per mole of 4-fluoroacetophenone, and an amount of a suitable solvent so that the total amount of the solvent in the mixture is from 550 to 1,660 ml per mole of 4-fluoroacetophenone; (c) adding to the mixture a seeding amount of crystals of Form I of 4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-lH-pyrazol-l-yl]-benzenesulfonamide based on 4-fluoroacetophenone; (d) collecting the Form I crystals
机译:(a)将每摩尔4-氟苯乙酮1.0-1.6摩尔三氟乙酸烷基酯,每摩尔4-氟苯乙酮1.0-1.5摩尔金属醇盐和已知量的4-氟苯乙酮混合以形成混合物; (b)将步骤(a)的混合物与每摩尔4-氟苯乙酮415至1,245毫升水,每摩尔4-氟苯乙酮1.1至2.0摩尔浓盐酸,0.8至1.2摩尔4-氯的混合物合并每摩尔4-氟苯乙酮盐酸盐磺酰氨基苯肼盐酸盐和合适的溶剂的量,使得混合物中溶剂的总量为每摩尔4-氟苯乙酮550-1,660ml; (c)向混合物中加入基于4-氟苯乙酮的4- [5-(4-氟苯基)-3-(三氟甲基)-1H-吡唑-1-基]-苯磺酰胺的晶型I的晶种; (d)收集I型晶体

著录项

  • 公开/公告号IN2010DN03525A

    专利类型

  • 公开/公告日2012-04-27

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN3525/DELNP/2010

  • 发明设计人 CHANGQUAN CALVIN SUN;GARRY O CONNOR;

    申请日2010-05-19

  • 分类号C07D231/12;

  • 国家 IN

  • 入库时间 2022-08-21 17:24:25

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