The synthesis and hypnotic evaluation of a new generation of thiazolo[3,2-a][1,3]diazepine analogs are described. Those compounds exhibit potent in vivo activities as ultra-short acting hypnotics. Background of the Invention Surgical procedures require the administration of several intravenous drugs to ensure hypnosis, analgesia, relaxation and control of visceral reflex responses. The use of i...

The method cited in the literature for synthesis of 1,2- dihydro 3- thioxo - 1,2,4- benzotriazine 1 was improved .1 was condensed with propargyl bromide to afford 3 - propargylthio – 1,2,4 -benzotriazine 5. Transformation of this compound to 9H-3- methylthiazolo [2,3-c] [1,2,4] benzotriazine ( 3, R = Me) was performed in the presence of Na O Me / MeOH . Orientation of this selective cy...

Oxazolo[5,4-f]quinoxalines, thiazolo[5,4-f]quinoxalines and pyrazino[b,e]isatins were all obtained from 5-iodo-6-aminoquinoxalines. While the first two families synthesized by nitrogen functionalization subsequent copper-catalyzed cyclization, latter was Sonogashira coupling, alkyne hydration, oxidative cyclization. Most of polycycles evaluated in biological tests.

The course of the four-component reactions of (2-benzimidazolyl) acetonitrile, carbondisulfide, isothiocyanate, and sulfur and selenium, respectively, is quite different. Whereas in the case of sulfur a tetracyclic [1,3]thiazolo[4 ,5 :4,5]pyrimido[1,6-a]benzimidazol-2(3H)-thione is formed, a zwitterionic 7-(benzimidazolium-2-yl)-[1,2]thiaselenolo[2,3-b][1,2,4]thiaselenazole-6-thiolate (an azase...