摘要
目的优选卡比多巴合成过程中脱甲基反应的工艺条件,确定最佳的生产工艺。方法以甲基多巴为原料经甲基化、酰胺化,再经降解、脱甲基得到卡比多巴。在最后一步脱甲基反应中,采用四因素三水平的正交设计试验,以卡比多巴收得率为评价指标,优选其工艺条件。结果确定的脱甲基最优工艺条件是加入10倍量的浓盐酸,反应时间为3.5 h。结论优选出的工艺条件操作简单、经济合理、便于控制,为工业化生产提供了实验依据。
Objective Optimization the demethylation reaction conditions in the process of synthesizing carbidopa, to determine the optimal production process. Methods With methyldopa as raw material, by methylation,amidation,fol-lowed degradation,demethylation,and then to obtain carbidopa. In the last step of demethylation reaction,with car-bidopa yield as the evaluation index,using four factors and three levels orthogonal design,to optimize the process con-ditions. Results The optimal process conditions for demethylation that is to add 10-fold amount of 36%（g/mL） hy-drochloric acid, and the reaction is remained for 3.5 hours. Conclusion The optimum process is simple,economical, reasonable and convenient for controlling. This study provide experimental basis for industrial production.
出处
《中国现代医生》
2014年第18期58-59,62,共3页
China Modern Doctor
基金
浙江省高技术产业发展计划(萧发改[2006]35号)
关键词
卡比多巴
合成工艺
正交设计
Carbidopa
Synthesis process
Orthogonal design
