2H-1,2,4-苯并噻二嗪-1,1-二氧类化合物的简便合成

2H- 1 ,2 ,4 -苯并噻二嗪 - 1 ,1 -二氧类化合物在药物化学中有广泛的应用。常作为利尿剂 ,促进肾脏对尿的排泄 ,和其他药物混合使用还具有一定的降压作用 ,常作为高血压病的辅助治疗药物。本世纪五十年代发现的氯噻嗪 ( )和双氢氯噻嗪( ) ,利尿作用很强 ,成为利尿药和降压药的重大突破。此外这类化合物还具有抗菌、消炎、刺激毛发生长 1] 等作用。在这类化合物的合成中 ,关环反应是关键步骤 ,文献报道过的主要方法为 :( 1 )用甲酸或原甲酸乙酯关环 2 ] ;( 2 )用醛关环 3 ] ;( 3)高温 (～ 2 0 0℃ )关环4] 。当磺酰胺 (氮 )上的氢未…

A CONVENIENT SYNTHESIS OF 2H-1,2,4-BENZOTHIADIAZINE-1,1-DIOXIDES

H 1,2,4 Benzothiadiazine 1,1 dioxide derivatives have been widely used in pharmaceutical chemistry.The formation of thiazide ring is a key step for preparing these compounds.Here we described a novel synthesis of the titled compounds in which the thiazide ring is formed conveniently by employing phosphorus oxychloride as dehydrating agent.The structures of the products were characterized by means of elemental analysis, 1HNMR,IR and ultraviolet spectra etc.The total yields of the titled compounds are above 45 percent.