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    • 7. 发明授权
    • Preparation of 2-alkylsulphonylalkylenepyrimidines
    • 2-烷基磺酰基亚苄基嘧啶的制备
    • US4754035A
    • 1988-06-28
    • US914439
    • 1986-10-02
    • Michael ArndtJosef Heinrich
    • Michael ArndtJosef Heinrich
    • C07D239/36C07D239/52C07D239/32C07D239/34C07D239/46
    • C07D239/36C07D239/52
    • A process for the preparation of a 2-alkylsulphonylalkylenepyrimidine optionally substituted in 5- and/or 6-positions of the formula ##STR1## comprising (1) reacting an ammonium halide, alkylmercaptan and chloroalkylenenitrile in the presence of an acid acceptor; (2) mixing an ester with an alkyl acetate in the presence of an alcoholic alcoholate solution and an inert diluent; mixing (1) and (2); after completion of reaction removing the alcohol; adding water and an acid to the residue; optionally concentrating the mixture; and, without further purification and/or isolation, reacting the mixture with hydrogen peroxide at a temperature between approximately -20.degree. C. and +100.degree. C. in the presence of a catalytic amount of a vanadium, tungsten or molybdenum salt, in the presence of water as a diluent.
    • 一种制备任选在式(VI)的5-和/或6-位上取代的2-烷基磺酰基亚烷基嘧啶的方法,包括(1)在酸受体存在下使卤化铵,烷基硫醇和氯代亚烷基腈反应; (2)在醇醇化物溶液和惰性稀释剂的存在下,将酯与乙酸烷基酯混合; 混合(1)和(2); 反应完成后除去醇; 向残渣中加入水和酸; 可选地浓缩混合物; 并且在不经进一步纯化和/或分离的情况下,在催化量的钒,钨或钼盐的存在下,在约-20℃至+ 100℃的温度下使混合物与过氧化氢反应, 存在水作为稀释剂。