Synthetic Route of 1082745-50-3,Some common heterocyclic compound, 1082745-50-3, name is 5-Amino-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxamide, molecular formula is C9H14N4O2, 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-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxamide (1.0 g, 4.76 mmol) and triethyl orthoformate (7.72 g, 47.6 mmol) in DMSO (20 mL) was added Cs2CO3 (3.1 g 9.5 mmol). The mixture was stirred at 130 C. for 36 hours. The mixture was diluted with water (100 mL) and extracted with DCM (30 mL*3). The organic layer was washed with water (30 mL*2) and dried over Na2SO4. The organic layer was evaporated under vacuum. The mixture was purified by silica gel chromatography (DCM: MeOH from 20:1 to 5:1) to give 6-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (560 mg, 50% yield).
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-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxamide, its application will become more common.
Reference:
Patent; H. Lundbeck A/S; Juhl, Karsten; Jessing, Mikkel; Langgard, Morten; Vital, Paulo Jorge Vieira; Marigo, Mauro; Kehler, Jan; Rasmussen, Lars Kyhn; (27 pag.)US2017/291901; (2017); A1;,
Pyrazole – Wikipedia,
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