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目的:探索雷莎吉兰不对称合成的新方法。方法:以1-茚酮为原料,经“一锅法”与R-叔丁基亚磺酰胺生成亚胺,后用NaBH4还原,经柱分离得到胺,再酸水解除去保护基得到R-1-氨基茚,再与丙炔氯结合,甲磺酸成盐得到雷莎吉兰。结果:经检测,所合成雷莎吉兰的旋光值,质谱,氢谱数据均与文献符合。结论:用手性的叔丁基亚磺酰胺合成手性胺是一种行之有效的方法,可运用在雷莎吉兰的合成中。
Objective: To explore a new method of asymmetric synthesis of rasagiline. Methods: 1-Indanone was used as raw material to produce imine by “one-pot method” and R-tert-butylsulfenamide. After reduction with NaBH4, the amine was separated by column and hydrolyzed to remove the protecting group R-1-amino-indene, then with propyne chloride, methanesulfonic acid salt to get rasagiline. Results: After detection, the data of optical rotation, mass spectrum and hydrogen spectrum of the synthesized rasagiline were in accordance with the literature. Conclusion: The chiral amine with chiral tert-butyl sulfenamide is an effective method and can be used in the synthesis of rasagiline.