With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.690261-64-4,2-(Piperidin-4-yl)pyrimidine hydrochloride,as a common compound, the synthetic route is as follows.
A solution of EDC.HCI (ALFA-AESAR, 340 mg, 1.77 mmol), TEA (ALFA-AESAR, 0.25 mL, 1 .77 mmol), HOBt (ALDRICH, 240 mg, 1 .77 mmol), Intermediate 30 (295.3 mg, 1.48 mmol) and 4,4,4-trifluorobutyric acid (ALFA-AESAR, 252 mg, 1.77 mmol) in DMF (15 mL) was stirred at rt overnight. The mixture was then washed with NaHCC>3 saturated solution and EtOAc was added, the two phases were separated and the aqueous one was further extracted with EtOAc. The collected organic layer was dried(anh) Na2SC>4, filtered and evaporated. The crude so obtained was purified by flash chromatography (Si SNAP 50, CyHex EtOAc from 1/1 to 0/10, then DCM/MeOH 8/2) to give title compound (141 mg, 33%) as a white solid. 1H NMR (500 MHz, DMSO-de) delta ppm: 8.75 (d, J = 4.9 Hz, 2H), 7.35 (t, J = 4.9 Hz, 1 H), 4.44 (d, J = 13.2 Hz, 1 H), 3.94 (d, J = 13.7 Hz, 1 H), 3.22-3.13 (m, 1 H), 3.13-3.05 (m, 1 H), 2.82-2.72 (m, 1 H), 2.70-2.57 (m, 2H), 2.57-2.45 (m, 2H), 2.02-1.90 (m, 1 H), 1.79-1.67 (m, 1 H),1.65-1.51 (m, 1 H). [ES+ MS] m/z 288 (MH+)., 690261-64-4
690261-64-4 2-(Piperidin-4-yl)pyrimidine hydrochloride 56965759, apiperidines compound, is more and more widely used in various fields.
Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BIOVERSYS AG; PORRAS DE FRANCISCO, Esther; REMUINAN-BLANCO, Modesto Jesus; BOUROTTE, Marilyne; DEPREZ, Benoit; WILLAND, Nicolas; (89 pag.)WO2019/34701; (2019); A1;,
Piperidine – Wikipedia
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