Studies On The Synthetical Technics Of Amlodipine

Amlodipine is the very representation of third-generation calcium channel blockers(CCB). it belongs to a family that called dihypropyridine. Amlodipine is mainly used for curing hypertensive and chest pain (angina). It has such advantages oflittle side effect ,lowers blood reposefully and very long half-time in blood plasma that permit patient only take medicine one time a day . it does not bring irritability tachycardia ,so, it is very prospective to cure the heartfailure .There are many routes to synthesis amlodipine in foreign patents. But some of them suffer from the supply of material, some of them suffer from the complicated manipulation. Some methods have problem that the hazardous material be used. On the basis of former people's research, we find a way to synthesis amlodipine that suits domestic condition. we study the reaction route deeply and roundly. The condition that affects all process was checked throughly , Such as ,solvent ,temperature, material ratio , catalyzer , reaction time , and disposing method. Further, we try to change something in order to get better result or a novel synthesic route .Not only we get the product that is accord with standard in higher yield , but, at least ,we get progress in two facets.First,we get a key intermediate (a) through a new way .The (a) that is synthesized by the new way is purer and cleaner than the one that was synthesized through the way described in literature . Second ,we use the mixture of aqueous methylamine and ethanol to deprotect . it not only shortens the reaction time but also represses the generation of side product.Now, we are also studying an intermediate(b) , based on it , a new way to synthesis amlodipine is undergoing.