Application of 180207-57-2, These common heterocyclic compound, 180207-57-2, name is 2-(1H-Pyrazol-4-yl)ethanol, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
2-(1H-pyrazol-4-yl)ethan-1-ol (300 mg, 2.7 mmol) was dissolved in DCM (10 mL), DIPEA (1.9 mL) was added and the solution cooled at 0 C. Methanesulfonyl chloride (620 DL, 8.3 mmol) was added, the solution was stirred for 1 h, then it was diluted with DCM (20 mL) and extracted with 10% aqueous citric acid (2×20 mL) and water (20 mL). The organic layer was dried over MgSO4 and filtered. The solvent was removed under reduced pressure and the crude was purified by chromatography (cyclohexane/EtOAc 0?100%) to afford 2-(1-(methylsulfonyl)-1H-pyrazol-4-yl)ethyl methanesulfonate (450 mg, 62%). 1H NMR (500 MHz, DMSO-d6) delta 8.20 (d, J = 0.8 Hz, 1 H), 7.92 (d, J = 0.8 Hz, 1 H), 4.39 (t, J = 6.6 Hz, 2H), 3.50 (s, 3H), 3.17 (s, 3H), 2.91 (t, J = 6.6, 0.9 Hz, 2H).
Statistics shows that 2-(1H-Pyrazol-4-yl)ethanol is playing an increasingly important role. we look forward to future research findings about 180207-57-2.
Reference:
Patent; THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL; MARAIS, Richard; SPRINGER, Caroline; NICULESCU-DUVAZ, Dan; MILLER, Natalie; ALJARAH, Mohammed; ZAMBON, Alfonso; LEUNG, Leo; SMITHEN, Deborah; BROWN, Michael; TANG, Haoran; (193 pag.)WO2019/73251; (2019); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics