Reacción #92659

Ecuación de reacción

BrCN

(S)-2-(4-phenoxyphenyl)-7-(piperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide

NaHCO3

water

→

white solid

Rendimiento 75.0%

(S)-7-(1-cyanopiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra hydropyrazolo[1,5-a]pyrimidine-3-carboxamide

Rendimiento 75.0%

Disolventes

brine

DCM

DCM

Condiciones de reacción

Tratamiento posterior

1. 1
   LavadoThe organic phase was further washed with brine (100 mL)
2. 2
   Secadodried over Na2SO4
3. 3
   ConcentraciónConcentrated
4. 4
   Otropurified by Pre-TLC (DCM/MeOH, 50/1)

Procedimiento

To a solution of (S)-2-(4-phenoxyphenyl)-7-(piperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide (417 mg, 1 mmol) in DCM (20 mL) was added NaHCO3 (168 mg, 2 mmol) and water (5 mL), followed by BrCN (127 mg, 1.2 mmol). The mixture was stirred at RT for 16 h. To the mixture was added DCM (50 mL) and brine (20 mL). The organic phase was further washed with brine (100 mL), dried over Na2SO4. Concentrated and purified by Pre-TLC (DCM/MeOH, 50/1) to afford 330 mg (75%) of white solid. MS (ESI) m/e [M+1]+ 443.0.

Fuente