2-氨基-3-氟吡啶的合成研究

Synthesis of 2-Amino-3-fluoro Pyridine

以2,3-二氟-5-氯吡啶为原料,通过氨基化、还原两步反应制备标题化合物。经正交试验优化,在反应温度为120℃、反应时间为24 h、投料比为1∶12的条件下,氨基化反应收率可达85.94%。该路线简单易操作、成本低廉,反应温和、后处理简单,适合工业化生产,路线总收率可达77.52%。

A simple and new synthetic approach to 2-amino-3-fluoropyridine was described. This method was started from 2,3-difluoro-5-chloropyridine, by amination,reduction of the two-step preparation of 3-fluoro-2-aminopyridine. After orthogonal test,when the reaction temperature was 120℃ ,reaction time was 24 h,the feed ratio was 1： 12, amination yield was 85.94% , the route is simple and easy operation, low cost, mild reaction, after-treatment is easy to operate and suitable for industrial production, the total yield was 77.52%.