6,7-亚甲二氧基-3-硫杂-1(2H,4H)吖啶酮的氨类衍生物及五元杂环并硫杂吖啶的合成

Amino Derivatives of Thio-acridon and Five-membered heterocyclesfused Thio-acridine

吖啶类化合物在抗疟和抗癌的药用研究中具有显著的作用[1,2],尤其在临床抗疟中广泛地应用了该类药物.

Some 6,7-Methylenedioxy-thio-1(2 H,4 H) acridine-fused heterocycles and ami-no derivatives of thio-acridone were synthesized.The title compound 1 reacted with hydrox-yamine hydrochloride to give the oxmine of 1 in good yiela.The oximc reacteu with variousacyl chloride to give the corresponding O-acyl-thio-acrioone oxime 4 a-c.The aooition ofisonicotan and arylhydrazine to 1 gave the hydrazone 2 b-f.Cyclization of led toindole-fused thia-acridine, a-c Reaction of with thiosemicarbazice gave pyrazole-fused thio-acridine (5),while pyrazoles 7-9 were obtained by condensation of hydrazine and diketoester 6.Furanodione and isoxazole-fusef thio-acridine (10 anf 11) were also synthesizedfrom diketo ester 6.-substituted thio-acridione (12) obtained by treatment of 6 with 1,2-diaminobenzene was converted to thio-acridine-fused furanoquinoxaline 1) in PPA.