目的优化雷沙吉兰甲磺酸盐合成工艺。方法 1-茚酮经一锅法还原-胺化制得1-氨基茚满,然后与3-溴丙炔反应得N-炔丙基-1-氨基茚满,用L-酒石酸拆分得R-(+)-N-炔丙基-1-氨基茚满酒石酸盐,最后碱化、成盐得雷沙吉兰甲磺酸盐。结果中间体及目标产物结构经~1H-NMR和MS确证结构,5步总收率达19.2%。结论此路线原料易得,反应条件温和,操作简便,收率高,适于工业化生产。 Objective To optimize the rasagiline mesylate synthesis process. The 1-indanone was reduced-aminated to produce 1-aminoindan, which was then reacted with 3-bromopropyne to obtain N-propargyl-1-aminoindan. The product was resolved by L-tartaric acid to give R - (+) - N-propargyl-1-aminoindan tartrate, and finally basified to form rasagiline mesylate. Results The structure of the intermediate and the target product were confirmed by ~ 1H-NMR and MS, and the total yield in 5 steps reached 19.2%. Conclusion This route is easy to obtain raw materials, mild reaction conditions, easy operation, high yield, suitable for industrial production.