Study On The Synthetic Technology Of Diltiazem

The pharmacological activity and clinical applications of Calcium Channel Blocker have been described in this paper. The action mechanism and Pharmacokinetic of Diltiazem have also been emphasized here. After the investigation, about two synthetic routes of Diltiazem, we have determined the better one for the goal of yield-increase, cost-cut and procedure-simplify, that the target compound Diltiazem Hydrochloric was obtained from p-methoxybenzaldehyde and Methyl chloroacetate for the raw material, through the Darzens condensation, S-alkylation, hydrolysis, resolution, cyclization, N-alkylation and O-acetylation. The synthetic technology has also been researched in detail. The overall yield has been increased to 13.6%, which was more 5.5% than that of the original literature method.Some kinds of resolution method have been investigated and the best one was chosen. The technologies of the recovery of the resolution reagents and the recycle of the undesired resolution products have been studied on in order to saving the raw material and lowering the cost, so that the yield of resolution has been increased to 48.3% from 34.0% that of the original literature method. At last, we determined a resolution technology which is most suitable to industrialization.