| 摘要 |
本发明系提供一种适合于工业上制造3,3-二甲基-3,4-二氢-1H-喹啉-2-酮衍生物的制造方法及用于该制造方法的合成中间体。;本发明系提供一种以式(1)所示的化合物或其盐的制造方法，式(1)[式(1)中，R 1 系表示氢原子、可具有取代基之烷基、可具有取代基之环烷基或可具有取代基之芳基，R 2 系表示氢原子、可具有取代基之烷基、羟基或氮原子的保护基，R 3 系表示氢原子、可具有取代基之烷基、羟基或氮原子的保护基，X系表示羟基或脱离基。]，其系包含：使式(2)[式(2)中，R 1 、R 2 及X系与式(1)中的定义相同，R 4 系表示可具有取代基之烷基、可具有取代基之环烷基或可具有取代基之芳基]所示的化合物或其盐、与硝化剂反应，以得到式(3)[式(3)中，R 1 、R 2 、R 4 及X系与式(1)及式(2)中的定义相同]所示的化合物或其盐之步骤，以及使前述式(3)所示的化合物或其盐还原，而得到前述式(1)所示的化合物或其盐的步骤。;The present invention provides a method for manufacturing a compound represented by formula (1) or a salt thereof, [in formula (1), R 1 represents hydrogen atom, an alkyl group which may have substituents, a cycloalkyl group which may have substituents or an aryl group which may have substituents, R 2 represents a hydrogen atom, an alkyl group which may have substituents, hydroxyl group or a protecting group of nitrogen atom, R 3 represents a hydrogen atom, an alkyl group which may have substituents, hydroxyl group or a protecting group of nitrogen atom, X represents hydroxyl group or a leaving group.], which includes: a step of reacting a compound represented by formula (2) or the salt thereof with a nitrification agent, [in formula (2), R 1 , R 2 and X have a same definition as in formula (1), R 4 represents an alkyl group which may have substituents, a cycloalkyl group which may have substituents, or an aryl group which may have substituents], to obtain a compound represented by formula (3) or the salt thereof, [in formula (3), R 1 , R 2 , R 4 and X have a same definition as in formula (1) and formula (2)], and a step of reducing the compound represented by formula (3) or the salt thereof, to obtain the compound represented by formula (1) or the salt thereof. |
