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    • 4. 发明授权
    • Processes for preparation of sulfonylurea derivatives
    • 制备磺酰脲衍生物的方法
    • US5525730A
    • 1996-06-11
    • US389042
    • 1995-02-15
    • Jong K. ChoiIn B. ChungJae C. LeeByoung W. SuhJong S. SaTae H. Heo
    • Jong K. ChoiIn B. ChungJae C. LeeByoung W. SuhJong S. SaTae H. Heo
    • C07D401/12A01N43/56B01J31/02C07B61/00C07D231/18C07D403/12C07D521/00
    • C07D521/00C07D231/18C07D401/12
    • The present invention relates to a novel process for preparing sulfonylurea derivatives of formula (I) in a high purity and a high yield characterized in that a sulfonylchloride of formula (V) is reacted with 2-amino-4,6-dimethoxypyrimidine of formula (VII) in the presence of a metal cyanate and an organic base catalyst or a compound of formula (VIII) is reacted with 2-amino-4,6-dimethoxypyrimidine of formula (VII): ##STR1## wherein R.sup.1 represents hydrogen, C.sub.1 -C.sub.4 alkyl or phenyl, R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, allyl or propargyl and R.sup.3 represents hydrogen, methyl, ethyl or phenyl, and to a process for preparing the sulfonylchloride compound of formula (V) above and the compound of formula (VIII) above, both of which are useful as an intermediate compound for preparing the sulfonylurea derivative of formula (I) and to a novel intermediate compound of formula (VIII) as defined above.
    • 本发明涉及以高纯度和高产率制备式(I)的磺酰脲衍生物的新方法,其特征在于式(Ⅴ)磺酰氯与式(Ⅴ)的2-氨基-4,6-二甲氧基嘧啶反应, VII)在金属氰酸盐和有机碱催化剂或式(VIII)化合物存在下与式(VII)的2-氨基-4,6-二甲氧基嘧啶反应:(I) V)表示氢,C 1 -C 4烷基或苯基,R 2表示氢,C 1 -C 4烷基,烯丙基或炔丙基,R 3表示氢,甲基,乙基或苯基,以及制备上述式(Ⅴ)磺酰氯化合物的方法 和上述式(VIII)化合物,它们都可用作制备式(I)的磺酰脲衍生物的中间体化合物和如上定义的新的式(Ⅷ)中间体化合物。