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目的对安立生坦合成工艺的改进进行研究。方法以二苯甲酮为起始原料,经过缩合、醇解、水解、拆分和取代反应合成安立生坦。醇解采用盐酸进行反应,采用拆分剂盐酸盐和碱试剂通过“一锅法”进行拆分。结果优化了醇解和拆分反应,避免了高毒性物质的产生;优化后,安立生坦的质量分数为99.7%,光学纯度达99.8%,工艺的总收率为30.0%。结论安立生坦的合成工艺改进后操作性好,条件温和,避免产生基因毒性和其他高毒性物质,成本较低,更适于药品的工业化生产。
OBJECTIVE To study the improvement of Anritsuantong synthesis process. Methods Benzophenone was used as the starting material to synthesize anritsyram by condensation, alcoholysis, hydrolysis, resolution and substitution reaction. Alcoholysis using hydrochloric acid for the reaction, the use of resolving agent hydrochloride and alkaline reagents through the “one-pot method” for resolution. The results optimize the alcoholysis and resolution reaction, to avoid the generation of highly toxic substances; after optimization, the concentration of the Anriconycins 99.7%, the optical purity of 99.8%, the total yield of 30.0%. Conclusions Anlisheng Tan has good operability and mild conditions to avoid genotoxicity and other highly toxic substances with low cost and is more suitable for industrialized production of drugs.