Reference of 82560-12-1, These common heterocyclic compound, 82560-12-1, name is 3-Amino-5-tert-butylpyrazole, its 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.
3-(tert-butyl)-lH-pyrazole-5-amine (503 mg, 3.61 mmol), Intermediate 30b (915 mg, 3.44 mmol), copper (I) iodide (32.8 mg, 0.172 mmol), trans- N,N’-dimethylcyclohexane- l ,2-diamine (97.8 mg, 0.688 mmol) and K2CO3 (998 mg, 7.22 mmol) were weighed in a round bottom flask, sealed with a septum and evacuated and purged with Ar 3 times. Xylene (4 ml, sparged with Ar for 45 min), was then introduced to the flask and the brown suspension was heated to 150C for 90 min. The reaction was cooled, diluted with EtOAc (10 mL), water (10 mL) and saturated aqueous NH4OH solution (5 mL). The aqueous layer was extracted with EtOAc (2 x 10 mL), and the combined organics washed with brine (15 mL), dried over Na2SO4, filtered, concentrated in vacuo and subjected to FCC eluting with 0 – 4% MeOH/EtOAc to afford the title compound as a pale yellow solid (457 mg, 48%). LCMS (Method 4): Rt 2.81 min, m/z 278 [MH+].
Statistics shows that 3-Amino-5-tert-butylpyrazole is playing an increasingly important role. we look forward to future research findings about 82560-12-1.
Reference:
Patent; CHIESI FARMACEUTICI S.P.A.; ALCARAZ, Lilian; PANCHAL, Terry Aaron; JENNINGS, Andrew Stephen Robert; CRIDLAND, Andrew Peter; HURLEY, Christopher; WO2014/194956; (2014); A1;,
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