We also applied our titanium catalytic system for the large-scale synthesis of tetrahydroquinoline-based crucial building blocks in an operationally simple manner. We predominantly conducted a range of 1-5 gram scale reactions with some selected quinolines and furnished the products 51a, 39a, 9a, and 26a in good yields, thereby enhancing the practicality of our method (Scheme 4). Scheme 4. Gram-scale reaction: See supporting information for the reaction procedure.