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在膀胱过度活动症治疗药米拉贝隆的合成工艺研究中发现易生成脱羟基副产物。为了对米拉贝隆的有关物质进行定量控制,本研究以苯乙酸和对硝基苯乙胺盐酸盐为原料,经酰胺缩合、硼烷还原、催化氢化后再与2-氨基噻唑-4-乙酸缩合,制得有关物质去羟基米拉贝隆盐酸盐,即2-(2-氨基噻唑-4-基)-N-[4-[2-(苯基乙基氨基)乙基]苯基]乙酰胺盐酸盐,并经MS、1H NMR和13C NMR确证结构。
In the overactive bladder treatment of Mirabene synthesis process studies found that easy to generate dehydroxylated by-products. In order to quantitatively control the related substances of mirabellone, phenylacetic acid and p-nitrophenethylamine hydrochloride were used as raw materials. After the amide condensation, borane reduction and catalytic hydrogenation, -acetic acid to give the related material, desmoparone hydrochloride, namely 2- [2-aminothiazol-4-yl) -N- [4- [2- (phenylethylamino) ethyl] Phenyl] acetamide hydrochloride and confirmed by MS, 1H NMR and 13C NMR.