利塞膦酸钠合成新工艺

New Synthesis Process of Risedronate Sodium

以烟酸为起始原料,经对甲基苯磺酸催化酯化、缩合、Willgerodt-Kindler反应、水解、酸化、膦酸化、成盐等步骤得利塞膦酸钠。优化后的工艺,在制备利塞膦酸的步骤中,加入活性炭作为分散剂,解决了双膦酸制备中放大反应后固化严重的问题,使工艺更适合工业化生产。

Risedronate sodium is synthesized from nicotinic acid via TsOH catalyzed esterification, con- densation, Willgerodt - Kindler reaction, hydrolysis, acidification, phosphine acidification, and formation of salt. The new process is more suitable for industrial production due to solving the solidification problem in the phosphine acidification step by adding activated carbon as the dispersing agent.