Reference of 1904-31-0,Some common heterocyclic compound, 1904-31-0, name is 1-Methyl-1H-pyrazol-3-amine, molecular formula is C4H7N3, 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.
2-Bromo-5-fluoropyridine (1) (1 .Og, 5.71 mmol), i-methyl-i H-pyrazol-3-amine (2) (554mg, 5.7immol), Xantphos (0.330g, 0.S7mmol), and 0s2003 (2.79g, 8.S6mmol) were combined in dry i,4-dioxane (i5mL). The reaction mixture was degassed with N2(g) and placed under vacuum for 10mm. Pd2(dba)3 (0.26ig, 0.28mmol) was then added and the resulting reaction mixture was heated at 9000 for 30h. It was then poured onto demineralized water (200mL), and extracted with EtOAc (3 x iOOmL). The organic phases were combined, dried over Na2SO4, filtered and subsequently concentrated in vacuo. The resulting residue was purified by flash chromatographywith EtOAc/Hexane (1:1) to provide 5-fluoro-N-(i -methyl-i H-pyrazol-3-yl)pyridin-2- amine (3) as a yellow solid (0.65g, 6ipercent).LCMS (ES): Found i93.0 [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 1-Methyl-1H-pyrazol-3-amine, its application will become more common.
Reference:
Patent; KARUS THERAPEUTICS LTD; SHUTTLEWORTH, Stephen Joseph; TOMASSI, Cyrille Davy; CECIL, Alexander Richard Liam; MACCORMICK, Somhairle; NODES, William John; SILVA, Franck Alexandre; WO2014/181137; (2014); A1;,
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