申请人:Societe de Conseils de Recherches et d'Applications Scientifiques
公开号:US04602020A1
公开(公告)日:1986-07-22
This invention relates to 1,3 - dihydro-6-aminomethyl-7-hydroxy-furo-(3,4-c)- pyridine derivatives of the general formula I ##STR1## wherein A.sub.1, A.sub.2, R.sub.1 and R.sub.2 represent various substituents, to pharmaceutically acceptable salts of such compounds, to a process for the preparation of compounds comprising reacting a 6-chloromethyl-7-benzoxy derivative of the general formula II ##STR2## with an excess of an amine derivative ##STR3## in a non-polar solvent, at a temperature not exceeding 20.degree. C., which leads to the desired substitution in position 6, followed by an acidic treatment to cleave the benzyl group and, finally to an anti-allergic composition of matter comprising, as an essential ingredient therein, an effective amount of one of these compounds together with an appropriate diluent or carrier.
本发明涉及一般式I的1,3-二氢-6-氨甲基-7-羟基呋喃(3,4-c)-吡啶衍生物,其中A.sub.1,A.sub.2,R.sub.1和R.sub.2代表各种取代基,以及这些化合物的药学上可接受的盐,制备这些化合物的过程包括在非极性溶剂中使用过量的胺衍生物II和6-氯甲基-7-苯甲氧基衍生物II的反应,反应温度不超过20℃,从而在位置6上得到所需的取代,随后进行酸性处理以裂解苯甲基,最终得到一种抗过敏物质组成,其中包括这些化合物的有效量和适当的稀释剂或载体。