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ChemicalBook CAS DataBase List 2-PHENYL-5-TRIFLUOROMETHYL-2H-PYRAZOL-3-YLAMINE

2-PHENYL-5-TRIFLUOROMETHYL-2H-PYRAZOL-3-YLAMINE synthesis

2synthesis methods
-

Yield:182923-55-3 13.4%

Reaction Conditions:

with acetic acid in ethanol at 85; for 12 h;

Steps:

77.2 Example 75: 4-chloro-1-phenyl-3-trifluoromethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide

To a solution of 3,3,3-trifluoro-2-oxopropionitrile (2.8 g, 20.7 mmol) in ethanol (40 mL), phenylhydrazine (2.24 g, 20.7 mmol) and HOAc (1 mL) was added. The mixture was stirred at 85 °C. for 12 hrs. The solvent was removed and the residue was dissolved in EA (50 mL), washed with NaHCO3 solution (30 mL) and brine (50 mL). The organic layer was separated and dried over anhydrous Na2SO4 The solvent was removed and the residue was purified by silica gel column (EA/PE = 1/10) to give 2-phenyl-5 -trifluoromethyl2H-pyrazol-3-ylamine (0.63 g, yield: 13.4%) as a yellow solid. ‘HNMR (400 MI-Tz, CDC13): = 7.56-7.49 (m, 4H), 7.44-7.42 (m, 1H), 5.86 (s, 1H), 3.92 (brs, 1H).

References:

WO2016/123392,2016,A2 Location in patent:Paragraph 00376