Related Products of 16034-46-1,Some common heterocyclic compound, 16034-46-1, name is 1-Methyl-1H-pyrazole-5-carboxylic acid, molecular formula is C5H6N2O2, 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.
DIPEA (370 )lL, 2.24 mmol) was added to a stirred solution of glycine methyl20 ester hydrochloride (70 mg, 0.56 mmol), 1-methyl-1H-pyrazole-5-carboxylic acid (71 mg,0.57 mmol) and HATU (255 mg, 0.67 mmol) in anhydrous DMF (1 mL) under a nitrogenatmosphere. The mixture was stirred at 20C for 15 h, then quenched by the addition ofsaturated aqueous sodium hydrogen carbonate solution (7 mL) and water (7 mL). Thematerial was extracted sequentially with ethyl acetate (3 x 7 mL) and 1:1 isopropanol/25 chloroform (2 x 7 mL). The combined organic layers were washed with brine (2 x 7 mL)and dried over sodium sulfate, then filtered and concentrated in vacuo. The residue waspurified by flash column chromatography, using a gradient of ethyl acetate in heptane (0-100%), to afford the title compound (110 mg, quantitative) as an orange-brown oil. DH(250 MHz, DMSO-d6) 8.92 (t,J5.6 Hz, 1H), 7.48 (d,J2.1 Hz, 1H), 6.89 (d,J2.1 Hz,30 1H), 4.04 (s, 3H), 3.98 (d, J 5.9 Hz, 2H), 3.66 (s, 3H). HPLC-MS (method 6): MH+ m/z198, RT 0.52 minutes.
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-pyrazole-5-carboxylic acid, its application will become more common.