申请人:Pfizer Inc.
公开号:US04175193A1
公开(公告)日:1979-11-20
The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxyquinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxyquinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxypyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.
在反应惰性溶剂存在碱的情况下,异烟酰亚胺与丙二腈反应,生成2-氨基-3-氰基-4-羟基喹啉和2-氨基-α,α-双氰乙酮,然后在酸性或碱性条件下水解和脱羧,生成2-氨基-4-羟基喹啉,作为制备1-氧代-1H-6-烷氧基嘧啶并[1,2-a]喹啉-2-羧酸和酯的中间体,具有抗过敏药物的价值。