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    • 2. 发明公开
    • PROCESS FOR PREPARING 2-ALKYL-3-AROYL-5-NITRO-BENZOFURANS
    • 制备2-烷基-3-芳酰基-5-硝基苯并呋喃的方法
    • EP2344467A1
    • 2011-07-20
    • EP08877230.6
    • 2008-10-10
    • Lonza Ltd.
    • WELLIG, AlainRODUIT, Jean-PaulDAI, DanmeiCHEN, Rongmin
    • C07D307/80C07C49/76
    • C07C45/673C07C45/455C07C45/71C07C251/52C07D307/80C07C49/84C07C49/825
    • The present invention relates to a process for the preparation of a compound of formula (I), wherein R
      1 is selected from C
      1-6 -alkyl, C
      3-6 -cycloalkyl and aralkyl, and wherein R
      2 at each occurrence independently is halogen or C
      1-6 -alkyl, and m is an integer from 0 to 4, Q is selected from halogen, -NO
      2 and -NR
      3 R
      4 , wherein R
      3 and R
      4 are independently selected from hydrogen, C
      1-6 -alkyl, C
      3-6 -cycloalkyl, aryl, aralkyl, mesyl and tosyl, or wherein R
      3 and R
      4 together form a C
      4-6 -alkylene group, Y at each occurrence is hydrogen or a hydroxy protection group W that can be hydrolytically cleaved under acidic conditions, and n is an integer from 1 to 3, and n is an integer from 1 to 3, with the proviso that n and m together are not greater than 5.
    • 本发明涉及制备式(I)化合物的方法,其中R 1选自C 1-6 - 烷基,C 3-6 - 环烷基和芳烷基,并且其中R 2在每次出现时独立地为 卤素或C 1-6 - 烷基,并且m是0至4的整数,Q选自卤素,-NO 2和-NR 3 R 4,其中R 3和R 4独立地选自氢,C 1-6 - 烷基,C 3-6 - 环烷基,芳基,芳烷基,甲磺酰基和甲苯磺酰基,或者其中R 3和R 4一起形成C 4-6 - 亚烷基,Y在每次出现时为氢或羟基保护基W, 在酸性条件下被水解裂解,并且n是1至3的整数,且n是1至3的整数,条件是n和m一起不大于5。