With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.845909-49-1,Ethyl 4-fluoropiperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.,845909-49-1
Intermediate B2(IIQ: 4-Fluoro-1 -(tetrahydro-pyran-4-yl)-piperidine-4-carboxylic acid ethyl esterTo a 250 mL RB were added compound B2(l) ethyl 4-fluoropiperidine-4- carboxylate, hydrochloride (1.25 g, 5.91 mmol, 1.0 eq), CH2CI2 (20 mL), 4- oxotetrahydropyranone B2(ll) (0.61 mL, 6.50 mmol, 1.10 eq), and glacial HOAc (0.340 mL, 5.91 mmol, 1.0 eq). After being stirred at rt for 5 to 10 min, sodium triacetoxyborohydride (2.02 g, 9.45 mmol, 1.60 eq) was added in one portion. A cloudy solution was obtained. After being stirred at rt for 12 h, the reaction mixture was diluted with 150 mL Et2O and 200 mL NaOH (1 M aqueous). The resulting suspension was stirred at rt for 1 h. The organic layer was collected, washed with 200 mL brine, dried over Na2SO4, filtered, and concentrated to afford 320 mg of the desired product, 4- fluoro-1-(tetrahydro-pyran-4-yl)-piperidine-4-carboxylic acid ethyl ester B2(IIO in 21 % yield as a colorless oil. 1H NNR (400 MHz, CDCI3, ppm) delta 1.30 (t, J = 7.08, 3H), 1.56- 1.66 (m, 2H), 1.74-1.78 (m, 2H), 1.94-2.21 (m, 4H), 2.46-2.55 (m, 3H), 2.82-2.85 (m, 2H), 3.38 (ddd, J = 1.52, 11.84, 11.84, 2H), 4.03 (dd, J = 4.28, 11.08, 2H), 4.24 (q, J = 7.05 Hz, 2H); 19F NMR (376 Hz, CDCI3, ppm) delta -166.94.
845909-49-1 Ethyl 4-fluoropiperidine-4-carboxylate hydrochloride 24729616, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; PFIZER INC.; WO2008/125945; (2008); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem