以水合肼作还原剂制备2-巯基-5-二氟甲氧基-1H-苯并咪唑

Using Hydrazine Hydrate as a Reductor for the Systhesis of 2-Mercapto-5-difluoromethoxy-1H-benzinidazole

以水合肼作还原剂,在Raney Ni催化下对2 硝基 4 二氟甲氧基苯胺进行还原;产物不经分离直接用于2 巯基 5 二氟甲氧基 1H 苯并咪唑的制备,总收率达到94%;操作简便,反应安全可靠,更适合于工业化生产.对水合肼的适用范围及催化剂的活性要求进行了试验,为寻找新的具有生理活性的质子泵抑制剂提供了一条安全、有效的途径.

2nitro4difluoromethoxyaniline was better reduced by using hydrazine hydrate in the presence of RaneyNi and followed by cyclocondensation with potassium ethylxanthate in one pot to give the 2mercapto5difluoromethoxy1Hbenzinidazole with an overall yield of 94%.In addition,the scope of application of the hydrazine hydrate and the active requirement of RaneyNi were considered showing that the process was simple and safe for industrialization.