Electric Literature of 112029-98-8,Some common heterocyclic compound, 112029-98-8, name is (1-Methyl-1H-pyrazol-4-yl)methanol, molecular formula is C5H8N2O, 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.
Step B 4-(methoxymethyl)-1-methyl-1,1-pyrazole To a suspension of sodium hydride (0.128 g, 3.21 mmol) in tetrahydrofuran (5 mL, 60 mmol) at 0° C. was added (1-methyl-1H-pyrazol-4-yl)methanol (0.300 g, 2.68 mmol) in tetrahydrofuran (2 mL, 20 mmol). The reaction was stirred at room temperature for 1 h, and then cooled down with ice bath. Methyl iodide (0.83 mL, 13 mmol) was added. The reaction was stirred at room temperature overnight. The reaction mixture was quenched with brine and extracted with EtOAc (3*). The combined organic phases were washed with water, brine, then dried over Na2SO4, and concentrated under reduced pressure to give 261 mg (77.2percent yield) of the desired product as colorless oil, which was directly used for the next reaction. LC/MS found: 127.2 (M+1)+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route (1-Methyl-1H-pyrazol-4-yl)methanol, its application will become more common.
Reference:
Patent; Incyte Corporation; Huang, Taisheng; Feng, Hao; Kong, Lingquan; Wang, Anlai; Ye, Hai Fen; US2013/96144; (2013); A1;,
Pyrazole – Wikipedia,
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