利福平化学合成环合反应体系水量控制的研究

Study on Controlling Water Content During the Cyclization Reaction for Synthesizing Rifampicin

有机合成反应的影响因素多,容易产生副反应,直接影响主产物的得率。利福平合成反应过程中环合反应要求在无水条件先进行,而参加反应的原料之一的二羟甲基叔丁胺(DMB)在反应体系中会分解产生水,不利于环合反应的正进行,并且影响到合成反应的收率,控制利福平合成反应过程中环合反应体系中的水分是提高利福平合成总收率的关键之一。因此,本文对利福平合成的反应机理、合成工艺及工艺配套设备进行了较为详细的研究,获得了一系列有实际价值的数据和结论,对控制环合反应体系水分的研究取得了突破性的进展,使利福平合成收率得到了大幅度的提高。

The organic reaction is often impacted by many factors and some side reactions easily happen, which will impact on the yield. The cyclization reaction should carry out under anhydrous condition, but the raw material dihydroxy methyl tert-butyl amine can produce water in the reaction, which will have positive impact on the cyclization reaction and the yield; So during the cyclization reaction, in order to improve the rifampicin total yield, the critical point is controlling the water content. In the paper, the reaction mechanism, synthetic process and corollary equipments of rifampicin production were studied, some data and conclusion were obtained, which is real value for controlling water content during the cyclization reaction to improve the yield of rifampicin.