| 摘要 |
<p>PURPOSE:A dehydrogenative ring-opening reagent is allowed act on octahydro- spiro[1,3-dioxolane-2,5'-quinoline-2'-one], which is stable and readily producible, to enable easy, one-step production of the title compound which is used as a remedy for stenocardia or the like. CONSTITUTION:A compound of the formula (R is butylamino, alkylsulfonyloxy, arylsulfonyloxy, acyloxy, hydroxy, halogen) is allowed to react with a dehydrogenative ring-opening reagent such as 2,3-dichloro-5,6- dicyanobenzoquinone, palladium-carbon, phenyltrimethylammonium perbromide to give the compound of formula II. The reaction is usually conducted under cooling or at room temperature, but ranges from 100-200 deg.C, when palladium- carbon is employed. The dehydrogenative ring-opening reagent is gradually added dropwise, when it is liquid, but added as it is, or in the form of solution, when crystalline.</p> |
