Electric Literature of 130599-34-7, A common heterocyclic compound, 130599-34-7, name is 3-(4-(Trifluoromethyl)phenyl)-1H-pyrazol-5-amine, molecular formula is C10H8F3N3, 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-Amino-5-(4-trifluoromethyl-phenyl)-pyrazole-l-carboxylic acid tert-butyl ester3-Amino-5-(4-trifluoiOmethyl-phenyl)-pyrazole (2.0 g, 8.8 mmol, 1.0 eq) and KOH 4.5 M (15.7 mL, 70.5 mmol, 8.0 eq) were dissolved in DCM (70 mL), and di- tert-butyl dicarbonate (2.02 g, 9.2 mmol, 1.1 eq) was added; the mixture was stirred at room temperature until complete conversion was observed by LC-MS analysis. The organic phase was washed with saturated brine and evaporated; the crude was crystallized with CH3CN, to give 1.9 g of title product (yield 69%).C15H16F3N3O2
The synthetic route of 130599-34-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; SIENA BIOTECH S.P.A.; WYETH PHARMACEUTICALS; WO2008/87529; (2008); A1;,
Pyrazole – Wikipedia,
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