PROBLEM TO BE SOLVED: To provide a process for preparation of a 1,2-dihydroquinoline derivative with a glucocorticoid receptor binding activity or a salt thereof, and to provide an intermediate for preparation thereof.SOLUTION: In a process for preparation including a step of eliminating an Rgroup and an Rgroup from a compound represented by formula (5) (wherein each of Rand Ris a hydrogen atom), a compound obtained by the elimination step is made to react with a compound represented by formula (d) in the presence of a base.【課題】グルココルチコイド受容体結合活性を有する１，２－ジヒドロキノリン誘導体またはその塩の製造方およびその製造中間体の提供。【解決手段】式（５）で表される化合物から、Ｒ1基とＲ2基を脱離させる工程、上記脱離工程で得られ化合物（式（５）中、Ｒ１とＲ２が水素原子である）を塩基存在下で、式（ｄ）で表される化合物と反応させる。【選択図】なし
