Reacción #165065

Ecuación de reacción

4-bromopyrazole

trans-1,2-cyclohexanediamine

potassium carbonate

N-(3-iodo-pyridin-2-yl)-2,2-dimethyl-propionamide

→

title compound

Rendimiento 53.4%

N-(3-(4-Bromo-pyrazol-1-yl)-pyridin-2-yl)-2,2-dimethyl-propionamide

Rendimiento 53.4%

Disolventes

toluene

Condiciones de reacción

Tratamiento posterior

1. 1
   ConcentraciónThe reaction mixture was concentrated under a reduced pressure
2. 2
   OtroThe residue was purified by NH silica gel column chromatography (ethyl acetate:heptane=2:1)

Procedimiento

To a mixture of N-(3-iodo-pyridin-2-yl)-2,2-dimethyl-propionamide (380 mg, 1.2 mmol) described in Manufacturing Example 39-1-2 and toluene (10 mL) were added 4-bromopyrazole (160 mg, 1.1 mmol), copper (I) iodide (11 mg, 0.056 mmol), trans-1,2-cyclohexanediamine (26 mg, 0.22 mmol) and potassium carbonate (340 mg, 2.5 mmol) at room temperature, which was stirred overnight at 110° C. The reaction mixture was concentrated under a reduced pressure. The residue was purified by NH silica gel column chromatography (ethyl acetate:heptane=2:1) to obtain the title compound (190 mg, 52%).

Fuente