申请人:Sumitomo Chemical Company, Limited
公开号:US04096144A1
公开(公告)日:1978-06-20
1,4-Substituted-2(1H)-quinazolinone derivatives are prepared by contactng a 2-aminophenyl ketone derivative with an alkaline agent such as alkali metal, alkali metal hydride, alkali metal amide, etc., reacting the thus obtained metal salt of 2-aminophenyl ketone derivative with a reactive ester of alcohols, reacting the thus obtained 2-(N-mono-substituted amino)-phenyl ketone derivative with a lower alkyl haloformate or a benzyl haloformate, and reacting the thus obtained carbamate derivative with ammonia. The 1,4-substituted-2(1H)-quinazolinone derivatives have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects.
通过将2-氨基苯酮衍生物与碱性试剂(如碱金属、碱金属氢化物、碱金属酰胺等)接触,制备出1,4-取代的2(1H)-喹唑啉酮衍生物;然后将所得的2-氨基苯酮衍生物金属盐与醇的反应性酯反应,将所得的2-(N-单取代氨基)-苯基酮衍生物与较低的烷基卤代甲酸酯或苄基卤代甲酸酯反应,最后将所得的氨基甲酸酯衍生物与氨反应。这些1,4-取代的2(1H)-喹唑啉酮衍生物具有出色的药理特性,特别是具有抗炎和镇痛作用。