盐酸右美托咪定的合成

目的优化盐酸右美托咪定合成路线关键中间产物美托咪定(目标化合物1)的制备工艺条件,使其适合工业生产。方法以N-三甲基硅咪唑为起始原料,通过Friedel-Crafts烷基化反应合成制备化合物1,并对催化剂Lewis酸和反应溶剂进行优化以得到较高的收率。结果优化得到的最佳反应体系是BF3OEt2/CH2Cl2,Friedel-Crafts反应收率可达到66.3%,目标产物经红外光谱、核磁共振图谱和元素分析确证了结构。结论本方法的原料成本低且易得,反应条件温和,可应用于工业化生产。

Synthesis of dexmedetomidine hydrochloride

Objective To optimize the process of preparing medetomidine(1) for industrial production,which is an important intermediate of dexmedetomidine hydrochloride.Methods Improved Friedel-Crafts Reaction was employed to obtain compound 1 with N-(trimethylsilyl) imidazole(TMSI) as a raw material.Solvents and Lewis acid as catalyst were investigated for high yields.Results The optimal conversion ratio of Friedel-Crafts Reaction was achieved to be 66.3% with BF3OEt2/CH2Cl2 as the catalyst.The product was confirmed to be the right structure via IR,NMR and elemental analysis.Conclusion The research shows that it is possible to get access to a relatively cheap reactant and a reasonable high conversion rate for the target product.Therefore it may be a sustainable method for the large scale industrial production.