Related Products of 78208-72-7,Some common heterocyclic compound, 78208-72-7, name is Ethyl 3-isopropyl-1H-pyrazole-5-carboxylate, molecular formula is C9H14N2O2, 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.
NaH (1.23 g, 31.15 mmol) was dissolved in DMF (200 mL) under 2 atmosphere at 0 °C. To this solution was added ethyl 5-isopropylpyrazole-3-carboxylate (5.16 g, 28.33 mmol) in DMF (50 mL) over 10 min at 0 °C. After the addition, the r.m. was stirred for 10 min at 0 °C and then at r.t. for 40 min. 2,2,2-Trifluoroethyl trifluoromethanesulfonate (4.5 mL, 31.15 mmol) was subsequently added and the mixture was stirred at r.t. for 3 h. After this time the rm was quenched by addition of EtOH at 0 °C. Water was added to the mixture and the water layer was extracted with EtOAc. The organic layer was then washed with brine, dried (MgS04), filtered and concentrated in vacuo. The resulting crude was purified by flash column chromatography (silica; heptanes/EtOAc 100/0 to 60/40) to afford intermediate 42 (4.05 g, 54percent) and regioisomer intermediate 43 (1.52 g, 20percent).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Ethyl 3-isopropyl-1H-pyrazole-5-carboxylate, its application will become more common.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; BISCHOFF, Francois, Paul; VELTER, Adriana, Ingrid; ROMBOUTS, Frederik, Jan, Rita; DE CLEYN, Michel, Anna, Jozef; VAN BRANDT, Sven, Franciscus, Anna; GIJSEN, Henricus, Jacobus, Maria; ZAVATTARO, Chiara; VAN DEN KEYBUS, Frans, Alfons, Maria; WO2014/111457; (2014); A1;,
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