申请人:Riker Laboratories, Inc.
公开号:US04018780A1
公开(公告)日:1977-04-19
4-Hydroxy[1]benzothieno[3,2-f]quinoline-2-carboxylic acids and esters thereof are prepared by the reaction of an optionally substituted 2-aminobenzothiophene with dimethyl acetylenedicarboxylate followed by ring closure. The sulfur atom of the intermediate compounds in the process can be oxidized to oxide or dioxide state, then hydrolyzed to the acids, or first hydrolyzed to the acids and then oxidized, if desired. The acids are physiologically active as anti-allergic agents in the acid form or as salts.
4-羟基[1]苯并噻吩[3,2-f]喹啉-2-羧酸及其酯是通过将可选择取代的2-氨基苯并噻吩与乙炔二羧酸二甲酯反应后进行环合制备的。在这个过程中,中间体化合物的硫原子可以被氧化为氧化物或二氧化物状态,然后水解为酸,或者首先水解为酸,然后氧化,根据需要进行。这些酸在酸形式或盐的形式下作为抗过敏剂在生理上具有活性。