卡比多巴的合成工艺优选

摘要

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.%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。