Studyies On A New Antianginal Drug Ranolazine And Its Derivatives

The mechanism arousing angina disease and the development of study on antianginal drugs in the worldwide have been described in this paper. The mechanisms of action and the pharmokinetic of ranolazine have also been discussed. After investigating about several synthetic routes of ranolazine, we have determined the best route for the goal of cost-cut and carried out detailed research in each step of the synthetic technology. The overall yield has been increased to 48.2 %, was more 25.7 % than that of the original literature methods.The synthetic technology of N-(2, 6-dimethylphenyl)-2-(l-piperazine) -acetamide, an important intermediate for ranolazine, has been optimized by substituting piperazine monohydrochloride salt for piperazine. The original method needs excessive piperazine in order to avoid the bis-A'-substitution occurring. This method uses equal mole of piperazine monohydrochloride salt, so it not only achieved the goal of cost-cut but also raised the yield dramatically from 34.8 % to 61.3%.According to the structure characteristics and structure-affection relationship, seven novel derivatives of ranolazine have been designed and synthesized. The structures of all synthesized compounds have been confirmed by ^-NMR and MS.