Method for producing substituted phenylsulfonyl urea
    3.
    发明申请
    Method for producing substituted phenylsulfonyl urea 审中-公开
    取代苯磺酰脲的制备方法

    公开(公告)号:US20060004198A1

    公开(公告)日:2006-01-05

    申请号:US10511968

    申请日:2003-04-16

    IPC分类号: C07D43/02

    摘要: The invention relates to a preparation process for the compound (I) or a salt thereof where Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) monoesterifying a compound (II) where Hal=a halogen atom, giving (III), b) either b1) ammonolysing and phosgenating this compound to give (V) or b2) converting this compound with cyanate into (V) and c) converting the resulting compound (V) with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) into the compound (I) or a salt thereof. Some compounds (II) and some intermediates (VIII), stabilized with N-heteroaromatic compounds, of the compounds (V) are novel. The compounds (II) can be obtained from the corresponding sulfobenzoic acids by reaction with acid halides of sulfur or phosphorus in nonpolar organic solvents.

    摘要翻译: 本发明涉及其中Q,X *,Y,Z,R,R 1,R 2和R 2的化合物(I)或其盐的制备方法 其中包括a)其中Hal =卤素原子的化合物(II)的单酯化,得到(III),b)b1)氨解和光气化该化合物,得到( V)或b2)将该化合物与氰酸酯转化为(V),和c)将所得化合物(V)与氨基杂环H 2 N-Het(Het =如(I)中的杂环))转化成 化合物(I)或其盐。 化合物(V)的一些化合物(II)和一些由N-杂芳族化合物稳定的中间体(VIII))是新颖的。 化合物(II)可以通过在非极性有机溶剂中与硫或磷的酰卤反应从相应的磺基苯甲酸获得。