Реакция #88919

Уравнение реакции

diethylazodicarboxylate

5-(5-Amino-3-tert-butyl-pyrazol-1-yl)-2-chloro-phenol

2-(tetrahydro-pyran-2-yloxy)-ethanol

Ph3P

→

title compound

Выход 89.0%

5-tert-Butyl-2-{4-chloro-3-[2-(tetrahydro-pyran-2-yloxy)-ethoxy]-phenyl}-2H-pyrazol-3-ylamine

Выход 89.0%

Растворители

THF

Условия реакции

Обработка

1. 1
   Концентрированиеthe mixture concentrated in vacuo
2. 2
   ДругоеThe residue was purified by FCC

Методика

To a solution of 5-(5-Amino-3-tert-butyl-pyrazol-1-yl)-2-chloro-phenol (WO2011/154734A1, which is incorporated herein by reference, 340 mg, 1.28 mmol), 2-(tetrahydro-pyran-2-yloxy)-ethanol (0.26 mL, 1.92 mmol) and Ph3P (671 mg, 2.56 mmol) in dry THF (10 mL) was added diethylazodicarboxylate (0.41 mL, 2.56 mmol) and the mixture stirred for 10 min. Water (4 drops) was added and the mixture concentrated in vacuo. The residue was purified by FCC, using 0-50% EtOAc in cyclohexane, to give the title compound (450 mg, 89%). LCMS (Method 3): Rt 3.73 min, m/z 394 [MH+].

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