首页> 外国专利> A NOVEL PROCESS FOR THE PREPARATION OF N-(4-NITRO-2-SULFAMOYL-PHENYL)-MALONAMIC ACID METHYL ESTER AND N-(4-AMINO-2-SULFAMOYL-PHENYL)-MALONAMIC ACID METHYL ESTER

A NOVEL PROCESS FOR THE PREPARATION OF N-(4-NITRO-2-SULFAMOYL-PHENYL)-MALONAMIC ACID METHYL ESTER AND N-(4-AMINO-2-SULFAMOYL-PHENYL)-MALONAMIC ACID METHYL ESTER

机译:N-(4-硝基-2-磺酰基-苯甲基)-丙二酸甲基酯和N-(4-氨基-2-磺酰基-苯甲基)-丙二酸甲基酯的制备新方法

摘要

The present invention provides a novel method for preparing compounds N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, which are novel intermediates for preparing a key intermediate N-(4-methanesulfonylamino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, for the preparation of N-(3-{(1R,2S,7R,8S)-3-[(4-fluorophenyl)methyl]-6-hydroxy-4-oxo-3-azatricyclo[6.2.1.02,7]undec-5-en-5-yl}-1,1-dioxo-1,4-dihydro-16,2,4-benzothiadiazin-7-yl)methanesulfonamide, also known commercially as Setrobuvir, a compound useful in treating hepatitis C.
机译:本发明提供了制备化合物N-(4-硝基-2-氨磺酰基-苯基)-丙二酸甲酯和N-(4-氨基-2-氨磺酰基-苯基)-丙二酸甲酯的新方法。新的中间体,用于制备关键中间体N-(4-甲磺酰基氨基-2-氨磺酰基-苯基)-丙二酸甲酯,用于制备N-(3-{(1R,2S,7R,8S)-3-[( 4-氟苯基)甲基] -6-羟基-4-氧代-3-氮杂三环[6.2.1.02,7]十一--5-烯-5-基} -1,1-二氧代-1,4-二氢-16, 2,4-苯并噻二嗪-7-基)甲磺酰胺,也商用称为Setrobuvir,是一种可用于治疗丙型肝炎的化合物。

著录项

  • 公开/公告号EP2943468B1

    专利类型

  • 公开/公告日2017-03-01

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG;

    申请/专利号EP20140722717

  • 发明设计人 ZHU JIANG;

    申请日2014-01-13

  • 分类号C07C311/46;C07C311/39;C07C303/38;C07C303/40;

  • 国家 EP

  • 入库时间 2022-08-21 14:04:45

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