Synthesis Of Starting Matrials For New Anti-HBV Reagents

The chronic hepatitis B, a severe contagious disease, is induced by Hepatitis B virus (HBV). One of the important treatments of the chronic hepatitis B is to control Hepatitis B virus DNA duplication. Based on our previous discovery, we have synthesized two new compounds as starting materials for new anti-HBV reagents. They were synthesized as following:4-(Ethylcarbamoyl)phenyl-4-(phenyldiazenyl)benzoate and 4-(dimethylcarbamoyl)phenyl-4-(phenyldiazenyl)benzoate were yielded respectively from the reactions ofN-ethyl-4-hydroxybenzamide, 4-hydroxy-N, N-dimethylbenzamide with 4-(phenyldiazenyl)benzoyl chloride in the presence of NaH. The products were analyzed by IR and1H-NMR.Amides and their reactions are important in both organic chemistry and biochemistry because large number of bioactive compounds or their intermediates possess amide groups. The methanol derivatives of N-aryl substituted secondary amides are useful intermediates in medicinal chemistry and organic synthesis. We have developed a simple and efficient procedure for hydroxymethylation of N-aryl amides that possess peri-CH and amide group interaction.These compounds yielded respectively from the reactions of N-(naphthalen-1-yl)acetamide, N-(4-dimethylamino)naphthalen-1-yl)acteamide and N-(biphenyl-2-yl) acettamide with polyformaldehyde in the presence of K2CO3, PTC and chloroform,are N-(hydroxymethyl)-N-(naphthalen-1-yl)acetamide, N-(4-dimethylamino)naphthalen-1-yl)-N-(hydroxymethyl)acetamide and N-(biphenyl-2-yl)-N-(hyroxymethyl)acetamide.All of the products were characterized by IR and 1H-NMR.