利福霉素SV氧化制备利福霉素S工艺研究  

Preparation of rifamycin S by oxidation of rifamycin SV

作　　者：范若兰 陈葵[1] 朱家文 于丽君 FAN Ruo-lan;CHEN Kui;ZHU Jia-wen;YU Li-jun(East China University of Science and Technology,Shanghai 200237,China)

机构地区：[1]华东理工大学化学工程研究所,上海200237

出　　处：《化学工程》2018年第10期51-55,共5页Chemical Engineering(China)

摘　　要：利福霉素S是合成利福霉素类药物的重要中间体,在工业中以次氯酸盐氧化利福霉素SV制得。工厂以搪玻璃釜为反应设备避免氯离子腐蚀,但造成混合不均、反应物降解等问题。为使用高效不锈钢设备,实现利福霉素S的连续化制备,需寻找一种无氯氧化剂。经确定反应溶液,以利福霉素S收率为指标,对比无氯氧化剂氧化效果,认为Fe^(2+)/H_2O_2能有效催化氧化利福霉素SV。通过单因素实验优化反应参数,得出:在Fe^(2+)与初始利福霉素SV摩尔配比n(Fe^(2+))∶n(rif SV)_0=1∶200、温度T=283. 15 K、pH=3. 5稀硫酸溶液中,以25%n(rif SV)_0/min半间歇方式滴加H_2O_2时,反应为动力学一级反应,反应速率常数为0. 123 2 min^(-1),利福霉素S收率可达53. 09%。研究认为,在利福霉素S合成工艺中,Fe^(2+)/H_2O_2具有一定的工业开发价值。Rifamycin S,an important intermediate in the synthesis of rifamycin antibiotics,is manufactured from rifamycin SV oxidation with hypochlorite as an oxidant.In order to avoid the intergranular corrosion of chloride ion to stainless steel equipment,the glass lined reactors are used in industry.However,mixture unevenness and degradation due to the long-time treatment have showed up.To achieve continuous production of rifamycin S by using stainless steel reactors,a chloride-free oxidant is urgent to be explored.With the determination of solvent and comparison among different oxidants,Fe 2+/H 2O 2 were chosen.Based on single-factor experiments,the reaction parameters were discussed and optimized.When the molar ratio of Fe 2+and rifamycin SV(in the initial stage)was 1∶200,in pH=3.5 H 2SO 4 solution,T=283.15 K,with semi-batch addition of 1%H 2O 2 at speed of 25%n(rif SV)0/min,the results showed:the oxidation was approaching to first order reaction;the reaction constant was 0.123 2 min-1 and the activation energy was 10.874 0 kJ/mol;the yield of rifamycin S achieved 53.09%.In conclusion,Fe 2+/H 2 O 2 could be applied for further industrial development in the preparation of rifamycin S.

关 键 词：利福霉素SV 利福霉素S 工艺 催化 动力学 

分 类 号：TQ465[化学工程—制药化工]