普鲁卡因胺最初是用对硝基苯甲酰氯和二乙氨基乙胺缩合成硝基卡因胺,再经接触氢化制取。其后三十余年虽有数种合成路线报道,比较实用的方法,仍沿用最初的这个路线,只是还原方法和试剂有所不同。这个合成路线的主要问题是产品难于纯化,生产工艺有较大困难。 本合成路线系将对氨基苯甲酸和二乙氨基乙胺在无溶剂无活化剂或脱水剂存在下熔融脱水制取普鲁卡因胺,蒸馏沸点为240°G/2mm,收率65％。如不经蒸馏制成水合物,洗去色质及杂质,二步总收率67％。普鲁卡因胺及其水合物均可在水中成盐,减压浓缩至内温120～140℃,倾入无水乙醇中结晶和脱色,无需反复精制已能符合药典分析要求,作为针剂原料,纯度、熔点较高(重结晶二次熔点168～170℃),引潮性小,生产工艺简单安全,成本 Procaine amine was originally p-nitrobenzoyl chloride and diethylamine amino acid condensation into nitro-caine amine, and then prepared by contact with hydrogenation. Although more than thirty years after the reports of several synthetic routes, a more practical method is still followed by the original route, only the reduction method and reagents are different. The main problem with this synthetic route is that the product is difficult to purify and the production process is more difficult. The synthetic route is that p-aminobenzoic acid and diethylaminoethylamine are melted and dehydrated in the absence of a solvent-free activator or a dehydrating agent to prepare procainamide, the boiling point of which is 240 ° G / 2mm and the yield is 65%. If not made into a hydrate distillation, washing color and impurities, two-step total yield of 67%. Prussianamine and its hydrates can be salified in water, concentrated under reduced pressure to an internal temperature of 120 ~ 140 ℃, poured into anhydrous ethanol crystallization and bleaching, without repeated purification has been able to meet the requirements of pharmacopoeia, as a raw material for injection , High purity, high melting point (recrystallization secondary melting point 168 ~ 170 ℃), low tide, the production process is simple and safe, the cost