甲磺酸雷沙吉兰的合成

Synthesis of Rasagiline Mesylate

2,3-二氢-1-茚酮与手性辅基(R)-苯乙胺缩合得到(R)-(+)-N-(1-苯基乙基)-2,3-二氢茚-1-亚胺,经硼氢化钠不对称还原、氢解脱苄制得(R)-1-氨基茚满盐酸盐,再与3-溴丙炔缩合、成甲磺酸盐制得抗帕金森病药甲磺酸雷沙吉兰,总收率为9.5%。

Rasagiline mesylate, an antiparkinson drug, was synthesized from indanone by condensation with （R）-phenylethylamine to give （R）- （＋）-N-（1-phenylethyl）indan-l-ylidene amine, which was subjected to asymmetrical reduction and catalytic hydrogenolysis to give （R）-1-indanamine hydrochloride, followed by condensation with propargyl bromide and salt formation with an overall yield of 9.5 %.