Some common heterocyclic compound, 20154-03-4, name is 3-(Trifluoromethyl)-1H-pyrazole, molecular formula is C4H3F3N2, 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. Formula: C4H3F3N2
[00554] Intermediate 55a: ethyl 2-[3-(trifluoromethyl)pyrazol-1-yI]acetate[00555] A solution of 3-(trifluoromethyl)-1 H-pyrazole (75mg, 0.SSmmol) and potassium carbonate (228mg, 1 .6Smmol) were left to stir in MeCN (2mL) for 30 minutes before the addition of ethyl bromoacetate (0.O9mL, 0.83mmol). The reaction mixture was then heated to 60 °C and left to stir for 2 hours. The reaction mixture was quenched by the addition of water (2OmL) and extractedusing EtOAc (3 x 2OmL). The organic layers were combined, dried over Na2504, filtered andconcentrated in vacuo to give ethyl 2-[3-(trifluoromethyl)pyrazol-1-yl]acetate (1 20mg, 0.SSmmol,100percent yield) as a yellow oil which was used in the next step without further purification.1H NMR (CDCI3,400MHz) O/ppm: 7.55 (1H, dd, J= 2.3Hz, 0.9Hz), 6.59 (1H, d, J= 2.2Hz), 4.96 (2H,5), 4.25 (2H, q, J= 7.1Hz), 1.29 (3H, t, J= 7.1Hz).MS Method 2: RT: 1.58 mi m/z 223.1 [M+H]
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 20154-03-4, its application will become more common.