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苯胺及取代的苯胺和Meldrum’s acid在固相无催化剂条件下反应,合成了丙二酸单苯酰胺(1a ～1f),收率81.0 % ～92.2 %.化合物1a ～1f在Eaton试剂(五氧化二磷+甲基磺酸)或多聚磷酸为环化试剂的条件下发生Friedel-Crafts分子内环化反应,以63.2 % ～93.8 %和56.5 % ～81.3 %的收率方便地得到4-羟基喹啉-2-酮衍生物(2a ～2f).产物的结构通过IR,1HNMR和元素分析得以证实.
Aniline and substituted aniline were reacted with Meldrum’s acid in the absence of catalyst under solid state conditions to synthesize monobenzamide (1a ~ 1f) in yield of 81.0% ~ 92.2% .Compounds 1a ~ 1f were synthesized in Eaton’s reagent Friedel-Crafts intramolecular cyclization reaction occurs under Friedel-Crafts phosphomolybdic acid, phosphorus + methanesulfonic acid or polyphosphoric acid as cyclization reagent, and the yield of 4-hydroxyquinoline is conveniently obtained from 63.2% to 93.8% and 56.5% to 81.3% 2-one derivatives (2a ~ 2f). The structure of the product was confirmed by IR, 1HNMR and elemental analysis.