With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.25850-22-0,2,2-Dimethyltetrahydro-2H-pyran-4-amine,as a common compound, the synthetic route is as follows.
Step 3 : 6-(3- {[4-(2,2-Dimethyltetrahvdro-2h-pwan-4-yl)-3-oxopiperazm- 1 -yllcarbonvU -4-fluoro benzyl)-4,5-dimethylpyridazin-3(2H)-one trifluoroacetate (JJ3).To a 0.4 M solution containing the intermediate JJ2 (leq) and 2,2-dimethyltetrahydro-2H-pyran- 4-amine (1.5 eq) in MeOH, were added NaBH3(CN) (1.5 eq) and catalytic AcOH. The reaction was heated in a MW apparatus (100 0C , 7 min). After evaporation of the solvent the crude intermediate was dissolved in DMF, then HATU (2 eq) and DIPEA (2 eq) were added and the mixture heated in MW apparatus (120 0C, 10 min). The crude product was purified by preparative RP-HPLC using H2O (0.1% TFA) and MeCN (0.1% TFA) as eluents and the combined fractions were evaporated under reduced pressure to afford the title compound (JJ3). 1H-NMR (300 MHz, DMSO-d6, 300K) delta: 12.65 (IH, bs), 7.36-7.14 (3H, m), 4.79-4.54 (IH, m), 4.20-4.10 (lH,m), 3.95 (2H, s), 3.86-3.50 (4H, m), 3.46-3.14 (3H, m), 1.99 (6H, s), 1.69-1.35 (4H, m) 1.22-1.10 (6H, m). MS (ES). C25H3iFN4O4 required: 470, found 471 (M+H) +.
25850-22-0, The synthetic route of 25850-22-0 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; WO2009/63244; (2009); A1;,
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