一种制备盐酸西那卡塞的新方法

摘要

Amide(2) was prepared by substitution of (R)-( +)-1-(1-naphthyl)ethylamine with acry-lyl chloride. 2 was coupled with 3-(trifluoromethoxy)iodobenzene to giveα,β-unsaturated amide(3). Cinacalcet hydrochloride was synthesized in overall yield of 40% by reduction with H2/Pd-C and NaBH4-BF3 ·OEt2 orderly and salt formation with hydrochloric acid from 3, with the purity of 99. 5%and the ee value of 99. 9%. The structure was confirmed by 1 H NMR and 13 C NMR.%(R)-1-萘乙胺与丙烯酰氯发生亲核取代反应制得酰胺(2)；2与3-三氟甲基碘苯经Heck偶联反应制得α，β不饱和酰胺(3)；3经两次还原反应后再与盐酸成盐合成了盐酸西那卡塞，总收率40%，纯度>99.5%， ee值>99.9%，其结构经1 H NMR和13 C NMR确证。