| 摘要 |
Process comprises reacting a benzene deriv. of formula (I) with a dialkylamide (II) in the presence of a base at 150-300 deg. C; R1 = a leaving gp.; R2 = H, aliphatic hydrocarbyl, halogen, or an electron-attracting gp. with a non-mesomeric inductive effect; R3 = any substit., esp. H or a gp. at least as electron attracting as alkyl gps.; R4 = a gp. as defined for R2; R5 = a gp. as defined for R3; R6 = aliphatic hydrocarbyl, halogen or an electron-attracting gp. with a non-mesomeric inductive effect; provided that at least one of R1, R6 and R4 is an electron-attracting gp.Pref. (II) is a N,N-di(1-3C alkyl)formamide. Reaction of (I) with (II) is in the presence of a cuprous salt at 180-250 deg. C. Reaction of the prod. with (IV) is at 0-100 (esp. 0-50) deg. C, where (IV) is a halogen, SO2Cl2, PCl5, PCl3/Cl2, an alkyl hypochlorite, Cl2O or Br2O. Reaction of the prod. with NH3 or an amine is at 150-250 (esp. 180-220) deg. C in the presence of a pyridine hydrohalide.
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