首页> 外国专利> PROCESS FOR THE PREPARATION OF POTASSIUM AND SODIUM SALTS OF N-PYRIDYL SULFONYL-N' PYRIMIDINYL UREAS, AND NOVEL POTASSIUM AND SODIUM SALTS OF 2-AMINOCARBOXYLAMINO-4, 6-DIMETHOXYPYRIMIDINE INTERMEDIATES THEREOF

PROCESS FOR THE PREPARATION OF POTASSIUM AND SODIUM SALTS OF N-PYRIDYL SULFONYL-N' PYRIMIDINYL UREAS, AND NOVEL POTASSIUM AND SODIUM SALTS OF 2-AMINOCARBOXYLAMINO-4, 6-DIMETHOXYPYRIMIDINE INTERMEDIATES THEREOF

机译:N-吡啶基磺酰基-N'嘧啶脲的钾钠盐的制备方法以及2-氨基羧酰胺基-4、6-二甲氧基嘧啶的新型钾钠盐的中间体

摘要

N-Pyridylsulphonyl-N'-pyrimidinylurea sodium and potassium salts (I) are produced from a pyrimidinyl isocyanate (IV) either by reaction with a pyridyl sulphonamide salt (V) or by reaction with ammonia, conversion of the resulting new pyrimidinylurea (III) into a new pyrimidinylurea sodium or potassium salt (II) and reaction of this salt with a pyridylsulphonyl chloride (VI). Production of N-pyridylsulphonyl-N'-pyrimidinylurea sodium and potassium salts of formula (I) comprises: (A) reacting 4,6-dimethoxypyrimidine-2-isocyanate of formula (IV) with a pyridin-2-yl sulphonamide salt of formula (V) in an aprotic solvent; or (B) reacting (IV) with ammonia in an aprotic solvent, treating the resulting 2-aminocarbonylamino-4,6-dimethoxy-pyrimidine of formula (III) with sodium or potassium hydride, hydroxide, hydrogen carbonate or carbonate or a sodium or potassium alcoholate in an aprotic solvent and reacting the 2-aminocarbonylamino-4,6-dimethoxy-pyrimidine sodium or potassium salt of formula (II) obtained with a pyridin-2-yl sulphonyl chloride (VI). R1 = CO2CH3; CON(CH3)2; OCH2CF3; N(CH3)COCH3; N(CH3)SO2CH3; CF3; or SO2C2H5; R2 = H or CF3; M = Na or K. Independent claims are also included for 2-aminocarbonylamino-4,6-dimethoxy-pyrimidine (III) and its Na and K salts (II).
机译:N-吡啶基磺酰基-N'-嘧啶基乙脲钠盐和钾盐(I)由嘧啶基异氰酸酯(IV)与吡啶基磺酰胺盐(V)反应或与氨反应,生成的新嘧啶基脲(III)转化而得生成新的嘧啶基脲钠盐或钾盐(II),并使该盐与吡啶基磺酰氯(VI)反应。式(I)的N-吡啶磺酰基-N'-嘧啶基乙脲钠和钾盐的生产包括:(A)使式(IV)的4,6-二甲氧基嘧啶-2-异氰酸酯与式(2)的吡啶-2-基磺酰胺盐反应(V)在非质子溶剂中;或(B)在非质子传递溶剂中使(IV)与氨反应,用氢化钠或氢化钾,氢氧化物,碳酸氢盐或碳酸盐或钠或氢氧化钠处理式(III)的2-氨基羰基氨基-4,6-二甲氧基-嘧啶在非质子传递溶剂中将乙醇酸钾溶液化,并使式(II)的2-氨基羰基氨基-4,6-二甲氧基-嘧啶钠或钾盐与吡啶-2-基磺酰氯(VI)反应。 R1 = CO2CH3; CON(CH3)2; OCH2CF3; N(CH3)COCH3; N(CH3)SO2CH3; CF3;或SO2C2H5; R2 = H或CF3; M = Na或K。还包括2-氨基羰基氨基-4,6-二甲氧基-嘧啶(III)及其Na和K盐(II)的独立权利要求。

著录项

  • 公开/公告号IL125952A

    专利类型

  • 公开/公告日2003-01-12

    原文格式PDF

  • 申请/专利权人 NOVARTIS AG;

    申请/专利号IL19980125952

  • 发明设计人

    申请日1998-08-27

  • 分类号C07D239/545;C07D401/12;

  • 国家 IL

  • 入库时间 2022-08-22 00:02:41

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