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    • 3. 发明申请
    • A NEW PROCESS FOR PREPARING 4- [4-METHYL-5- (CL- 10ALKYLTHIO/C5-10ARYL-CL-6ALKYLTHIO) -4H-1, 2, 4-TRIAZOL-3- YL] PYRIDINES.
    • 用于制备4- [4-甲基-5-(CL-十二基甲硅烷基)/ C 5-10] -L-六烯基)-4H-1,2,4-三唑-3-基]吡啶的新方法。
    • WO2010068172A1
    • 2010-06-17
    • PCT/SE2009/051404
    • 2009-12-11
    • ASTRAZENECA ABÅSTRÖM, HansJONES, ElfynSTÅHLBERG, Tim
    • ÅSTRÖM, HansJONES, ElfynSTÅHLBERG, Tim
    • C07D401/04C07D249/12
    • C07D401/04
    • The invention relates to a method of manufacturing a compound according to formula (I) wherein R is C 1-6 alkylor C 5-10 aryl-C 1-6 alkyl, comprising the steps of: a) reacting isonicotinohydrazide and methyl isothiocyanate, thereby obtaining 2-isonicotinoyl-N-methylhydrazinecarbothioamide; b) under alkaline conditions allowing said 2-isonicotinoyl-N-methylhydrazinecarbothioamide to undergo a ring-forming reaction, thereby obtaining 4-methyl-5-pyridin-4-yl-2,4-dihydro-3H-1,2,4-triazole-3-thione; and c) under alkaline conditions allowing said 4-methyl-5-pyridin-4-yl-2,4-dihydro-3H-1,2,4-triazole-3-thione to react with R-X, wherein R has the same meaning as in formula I and X is selected from the group of Cl, Br and I, thereby obtaining a compound according to formula I; wherein steps a), b) and c) are carried out in an aqueous environment without intermediate isolations.
    • 本发明涉及一种制备式(I)化合物的方法,其中R为C 1-6烷基或C 5-10芳基-C 1-6烷基,包括以下步骤:a)使异烟酰肼与异硫氰酸甲酯反应,得到2-异烟酰基-N -methylhydrazinecarbothioamide; b)在碱性条件下,使所述2-异烟酰基-N-甲基肼硫代硫酰胺进行成环反应,从而得到4-甲基-5-吡啶-4-基-2,4-二氢-3H- 三唑-3-硫酮; 和c)在碱性条件下,使所述4-甲基-5-吡啶-4-基-2,4-二氢-3H-1,2,4-三唑-3-硫酮与RX反应,其中R具有相同的含义 如式I所示,X选自Cl,Br和I组,由此得到式I化合物; 其中步骤a),b)和c)在没有中间隔离的水性环境中进行。