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    • 16. 发明申请
    • Method for production of aryl-substituted annelated pyrimidines
    • 芳基取代的环状嘧啶的制备方法
    • US20100087640A1
    • 2010-04-08
    • US12521877
    • 2008-01-10
    • Bernd WolfVolker MaywaldMichael KeilManuel BudichMichael RackManfred Ehresmann
    • Bernd WolfVolker MaywaldMichael KeilManuel BudichMichael RackManfred Ehresmann
    • C07D487/04
    • C07D487/04
    • The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.
    • 本发明涉及制备通式(I)的芳基取代的稠合嘧啶的方法,其中L 1至L 5为H,卤素,CN,NO 2,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 1 -C 4 - 烷氧基,C1-C4-卤代烷氧基等; Y1至Y3为C-RY或N; RY为H或任选取代的C 1 -C 4烷基或两个相邻的RY一起形成环; X是OH,Cl或Br; 其包括(i)2-苯基丙二酸酯与化合物(III)或其互变异构体在合适的碱的存在下反应,其中反应期间释放的醇与式R-OH的连续从 减压下的反应混合物; 得到其中X是OH的式(I)化合物或其盐,并且如果通式(I)的化合物中的X是氯或溴,则(ii)式(I)化合物 I)或与卤化剂的盐。