Electric Literature of 1384973-12-9,Some common heterocyclic compound, 1384973-12-9, name is 5-Amino-3-bromo-1H-pyrazole-4-carbonitrile, molecular formula is C4H3BrN4, 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.
To a solution of 5-amino-3-bromo-lH-pyrazole-4-carbonitrile (500 mg, 2.67 mmol) in EtOH (5 mL)/H20 (5 mL) /toluene (5 mL) were added 3 -pyridine boronic acid (493 mg, 4.01 mmol), K3P04 (2.13 g, 8.02 mmol) and Pd(dppf)Cl2 (391 mg, 0.53 mmol) under N2. The resulting mixture was stirred at 110C for 64 hours under N2. After cooling to rt, the mixture was concentrated in vacuo, diluted with ethyl acetate, washed with water (10 mL x 3) and dried over MgS04. After filtration, the filtrate was concentrated in vacuo. The residue was purified by preparative-TLC to afford 300mg of the desired product: MS (m/z): 185.9 [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 5-Amino-3-bromo-1H-pyrazole-4-carbonitrile, its application will become more common.