Reacción #1135840

Ecuación de reacción

N1-cyclopropylbenzene-1,2-diamine

triethylamine

methyl 8-chloro-8-oxooctanoate

→

methyl 8-(2-(cyclopropylamino)phenylamino)-8-oxooctanoate

Rendimiento 94.2%

Disolventes

ethyl acetate

DMF

DMF

Condiciones de reacción

Tratamiento posterior

1. 1
   Lavadowashed with 1 N HCl, saturated sodium bicarbonate solution and brine
2. 2
   ConcentraciónThe separated organic layer was concentrated

Procedimiento

To a solution of N1-cyclopropylbenzene-1,2-diamine (221 mg, 1.49 mmol) and triethylamine (0.3 mL, 2.2 mmol) in DMF was added a solution of methyl 8-chloro-8-oxooctanoate (260 mg, 1.3 mmol) in DMF at 0° C. drop-wise. The reaction was stirred overnight at room temperature, diluted with ethyl acetate and washed with 1 N HCl, saturated sodium bicarbonate solution and brine. The separated organic layer was concentrated to give crude methyl 8-(2-(cyclopropylamino)phenylamino)-8-oxooctanoate (390 mg)

Fuente