Reacción #70488

Ecuación de reacción

6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-nicotinic acid

Diisopropylethylamine

HBTU

2-(methylamino)ethanol

→

title compound

Rendimiento 61.0%

6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-N-(2-hydroxyethyl)-N-methyl-nicotinamide

Rendimiento 61.0%

Disolventes

DMF

Condiciones de reacción

Tratamiento posterior

1. 1
   ConcentraciónConcentrate
2. 2
   Otroto remove DMF in vacuo
3. 3
   OtroThe residue is purified by flash chromatography on silica gel (0-25% MeOH/CH2Cl2 with 5% TEA)

Procedimiento

6-{4-[4-(4-Fluoro-benzyl)-phthalazin-1-yl]-piperazin-1-yl}-nicotinic acid (100 mg, 0.225 mmol), DMF (0.5 mL), Diisopropylethylamine (195 μL, 1.125 mmol), HBTU (102 mg, 0.270 mmol), and 2-(methylamino)ethanol (18 μL, 0.225 mmol) are combined in a 10 mL flask and stirred for 4 h at room temperature. Concentrate to remove DMF in vacuo. The residue is purified by flash chromatography on silica gel (0-25% MeOH/CH2Cl2 with 5% TEA) to afford the title compound (68.2 mg, 61%).

Fuente