With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1245724-46-2,(S)-Tetrahydro-2H-pyran-3-amine hydrochloride,as a common compound, the synthetic route is as follows.
(S)-Tetrahydro-2H-pyran-3-amine hydrochloride (1.99 g, 14.48 mmol) in MeCN (10 mL) wasadded drop wise to a mixture of DIPEA ( 6.30 mL, 36.19 mmol) and ethyl 2,4-dichloropyrimidine-5-carboxylate (3.20 g, 14.48 mmol) in MeCN (60 mL) at 0C over a period of 5 min under air. Thereaction mixture was stirred for 4 h, slowly allowing to warm to rt, then was stirred at rt for 18 h5 and concentrated in vacuo, diluted with EtOAc (100 mL), and washed with water then with sat.brine. The organic layer was dried over MgS04, filtered and concentrated in vacuo, and purified byfcc, eluting with 0 – 40% EtOAc in n-heptane, to afford the title compound (3.24 g, 78%) as ayellow oil; 1H NMR (400 MHz, DMSO) 1.32 (3H, t), 1.49- 1.6 (lH, m), 1.63- 1.79 (2H, m), 1.83- 1.94 (lH, m), 3.48 (lH, dd), 3.54-3.65 (2H, m), 3.74 (lH, dd), 4.08-4.19 (lH, m), 4.33 (2H, q),10 8.57 (lH, d), 8.64 (lH, s); m/z [M-Hl284.
1245724-46-2, The synthetic route of 1245724-46-2 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; ASTRAZENECA AB; CANCER RESEARCH TECHNOLOGY LIMITED; FINLAY, Maurice, Raymond, Verschoyle; GOLDBERG, Frederick, Woolf; HOWARD, Martin, Richard; TING, Attilla, Kuan, Tsuei; (145 pag.)WO2019/238929; (2019); A1;,
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