With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.118511-81-2,1-(Piperidin-4-yl)-1H-indole,as a common compound, the synthetic route is as follows.
General procedure: To a solution of A (16.64 g, 52 mmol) in CH2Cl2 (45 mL) was added TFA (30 mL) slowly at rt. The mixture was stirred at rt for 3 h (monitor by HPLC). The mixture was concentrated to remove most of solvent and TFA. The crude product was partitioned in CH2Cl2/H2O (100 mL/50 mL) and stirred. Then, 3N NaOH(aq) was added slowly until the pH value of aqueous layer is >11. The aqueous layer was then extracted with CH2Cl2 (100 mL x 10). The combined CH2Cl2 layer was dried (Na2SO4) and filtered. After removal of solvent, the crude product (free base) was dissolved in Et2O (100 mL) and 1N HCl (1M in Et2O, 60 mL, 60 mmol) was added slowly at 0 C. Then, the mixture was allowed to warm to rt for another 30 min. Hexane (100 mL) was added and stirred for 15 min. The white solid was then filtered and washed with 50% Et2O/hexane (30 mL x 3) and dried to give 12.82 g of intermediate B (96%) as a white HCl salt.
118511-81-2, 118511-81-2 1-(Piperidin-4-yl)-1H-indole 14090755, apiperidines compound, is more and more widely used in various fields.
Reference：
Article; Yang, Shyh-Ming; Tang, Yuting; Rano, Thomas; Lu, Huajun; Kuo, Gee-Hong; Gaul, Michael D.; Li, Yaxin; Ho, George; Lang, Wensheng; Conway, James G.; Liang, Yin; Lenhard, James M.; Demarest, Keith T.; Murray, William V.; Bioorganic and Medicinal Chemistry Letters; vol. 24; 5; (2014); p. 1437 – 1441;,
Piperidine – Wikipedia
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