Study On The Synthesis Of Recemic Ramosetron Hydrochloride

Ramosetron Hydrochloride,R-(1-methyl-1H-indol-3-yl) (4,5,6,7 -tetrahydro-1H -benzoimidazol-5-yl) methanone hydrochloride,one of 5-Hydroxytryptamine receptor antagonists. Yamanouchi Pharmaceu- tical. Co. Ltd. Tokyo. Japan.It was sailed first time in 1998 Japan. The medicine has been introduced into the market since 1998.And it has been used widely in clinic for curing naupathia and spew caused by malignancy.The medicine is excellent in high efficiency ,high security and low side-effect.All of these make it become one of the best new medicine for curing naupathia and spew at the present timeIn the research process of this paper, I firstly to many papers to find out the research background. The synthesis route of ramosetron hydrochloride was elaborately chsen.. First we separately synthesized pyrrolidin-1-yl (4.,5,6,7- tetrahydrobenzoimidazol–5-yl ) methanone and N-methylindole,then synthesized the recemic ramosetron hydrochloride at last.The syntheses of pyrrolidin-1-yl (4.,5,6,7- tetrahydro-benzo- imidazol-5-yl ) methanone are the key processes.It was synthesized from 3,4-diaminobenzoic acid as the starting material via getted ring , esterify,hydrogenation,hydrolyze etal five steps.In the hydrogenation reaction,we choosed mang catalysts solvents ,changed the reaction temperature and press.and then ,we try to do hydrogenation in mang different reaction.at last we make sure an reaction condition with reason.In the synthesis process of N-methylindole,the condition of the reaction was optimized, and the yield of product was improved.The intermediate pyrrolidin-1-yl(4,5,6,7-tetra-hydro-benzo imidazol -5-yl ) methanoneand the other intermediate N-methylindole was used to produce target compound recemic ramosetron hydrochloride.Through the work of this paper,the esperiments achieved the anticipative effect,which has accumulated the basic data for their industrial manufacturing.