Synethsis of Related Substance of Chlorpenamine
|School||Hebei University of Science and Technology|
|Keywords||Chloropenamine related substance synthesis antihistamine drug nucleophilc reaction|
To assure the safety and effectiveness is the basic principal of the research and evaluation of a new drug, and the stability and controllability of the drug is the basic requirement to reach these purposes. So the research of the purity of the drug is the important aspect of the quality research. In a word, the research of the purity is a systematic engineering, and has close relationship with process research, quality research, stability research, pharmacology and toxicology research, and connected with the quality and safety of the registered drug.As an anti-allergic drug, chlorpenamine has been used broadly in the clinic. In order to control the quality of chlorpenamine, four related substance named A, B, and C have been obtained by the synthetic method.Related substance A was obtained from4-chlorophenylacetonitrile and chloroamine hydrochloride, which was reacted under basic condition, and the yield was31%. Related substance B was obtained from4-chlorophenylacetonitrile and2-bromopyridine, which was reacted under basic condition, as reddish solid, and then substituted with chloroamine hydrochloride, and the yield was48.1%. Related substance C was obtained from chlorophenamine, which was condensed with ethyl chloroformate, and then hydrolyzed with methyl magnesium chloride, and the total yield was13.9%.