Some new pyridazinone derivatives(3) were synthesized through addition of antipyrin to β- aroylacrylic acids (1) followed by cyclization of the adducts. Reactions of 3 with ethyl bromoacetate, benzenesulfonyl chlorid...Some new pyridazinone derivatives(3) were synthesized through addition of antipyrin to β- aroylacrylic acids (1) followed by cyclization of the adducts. Reactions of 3 with ethyl bromoacetate, benzenesulfonyl chloride, benzoyl chloride and POCl_3 give N-substituted products and monochlorosub- stituted pyridazines (4), respectively. The reactions of the latter with thiourea give unexpected dithio- derivatives(5), which react with phenylhydrazine to give pyrazolopyridazino pyridazine derivatives (6). Reactions of 2 with NH_2OH in ethanol and pyridine afford oxime and oxazinone derivatives 7 and 8, tespectively. The antibacterial activities of several compounds were screened.展开更多
文摘Some new pyridazinone derivatives(3) were synthesized through addition of antipyrin to β- aroylacrylic acids (1) followed by cyclization of the adducts. Reactions of 3 with ethyl bromoacetate, benzenesulfonyl chloride, benzoyl chloride and POCl_3 give N-substituted products and monochlorosub- stituted pyridazines (4), respectively. The reactions of the latter with thiourea give unexpected dithio- derivatives(5), which react with phenylhydrazine to give pyrazolopyridazino pyridazine derivatives (6). Reactions of 2 with NH_2OH in ethanol and pyridine afford oxime and oxazinone derivatives 7 and 8, tespectively. The antibacterial activities of several compounds were screened.
