The present invention provides a method of preparing thieno[3,2-c]pyridine derivatives of formula I:
wherein R1 is selected from the group consisting of lower alkyl; lower alkylene phenyl; substituted lower alkylene phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro and halo; lower alkylene naphthyl, lower alkylene thienyl; lower alkylene diphenyl; lower alkylene-hydroxy-phenyl; substituted lower alkylene-hydroxy-phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro, and halo; lower alkylene-hydroxy-naphthyl; lower alkylene-hydroxy-thienyl; lower alkylene-hydroxy-diphenyl, and R2 is H or lower alkylene. The method comprises reacting a compound of a formula II:
with a cyclic dioxy or cyclic dithio in the presence of catalyst.
本发明提供了一种制备式 I 的噻吩并[3,2-c]吡啶衍生物的方法:
其中 R1 选自由低级烷基;低级亚烷基苯基;取代的低级亚烷基苯基,其中苯基被低级烷基、低级烷氧基、低级酰氧基、羟基、硝基和卤素取代 1 至 3 次;低级亚烷基萘基;低级亚烷基噻吩基;低级亚烷基二苯基;低级亚烷基羟基苯基;取代的低级亚烷基羟基苯基,其中苯基被低级烷基、低级烷氧基、低级酰氧基、羟基、硝基和卤素取代 1 至 3 次;低级亚烷基羟基萘基;低级亚烷基羟基噻吩基;低级亚烷基羟基二苯基,且 R2 为 H 或低级亚烷基。该方法包括将式 II:
与环二氧基或环二硫在催化剂存在下反应。