Three Mothods for Producing 4-Aminobenzamidine dihydrochloride

4-Aminobenzimididine dihydrochloride is a reagent that has attracted much attention. It is not only an important chemical raw material and pharmaceutical intermediate, but also an inhibitor of many enzymes such as trypsin and urokinase. This article will introduce three synthetic processes of 4-aminobenzamidine dihydrochloride.

In the first method, p-nitrobenzonitrile is subjected to amidation reaction in amidine reagent (sulfoxide chloride, phosphorus trichloride or phosphorus pentachloride) to obtain intermediate p-nitrobenzoimidate; then P-nitrobenzamidine is obtained by amidation reaction in an amidation reagent, and then under acidic conditions, it is reduced by a reducing agent in a mixed solvent of water and alcohol to obtain 4-aminobenzamidine dihydrochloride.

In the second method, starting from p-nitrobenzaldehyde, p-nitrobenzaldehyde and hydroxylamine hydrochloride form p-nitrobenzonitrile, and then react with ammonium salt to form p-nitrobenzamidine, which is then acylated, The reduction yields n-hexyl p-aminobenzamidine imine formate, and finally forms a salt with hydrogen chloride to obtain 4-aminobenzamidine dihydrochloride.

In the third method, para-acetaminobenzonitrile is dissolved in a solvent, and then a strong base with an ammonia source is added to react at a certain temperature. After the reaction is completed, hydrochloric acid is added to quench the reaction. After treatment, 4-aminobenzamidine dihydrochloride is obtained.

The above three 4-aminobenzamidine dihydrochloride production processes have the characteristics of easy availability of raw materials, controllable cost and simple operation. The third process is more exquisite, and the p-aminobenzamidine hydrochloride is obtained through a one-step chemical reaction, which not only further simplifies the operation process, the reaction time is short, but also the yield of the obtained 4-aminobenzamidine dihydrochloride is high, and the product Good purity and high quality, suitable for industrial production.

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