Reacción #362542

Ecuación de reacción

1-[1-(2-aminoethyl)-4-piperidyl]-3-(4-fluorophenyl)-5-methyl-1H-indole

1-[1-(2-Aminoethyl)-4-piperidyl]-3-(4-fluorophenyl)-5-methyl-1H-indole

K2CO3

methyl chloroformate

→

1-[1-(N-methoxycarbonyl-2-aminoethyl)-4piperidyl]-3-(4-fluorophenyl)-5-methyl-1H-indole

Disolventes

dichloromethane

dichloromethane

Condiciones de reacción

Tratamiento posterior

1. 1
   Temperaturawas cooled to 0°-5° C.
2. 2
   OtroAfter reaction for further 2 h at room temperature the reaction mixture
3. 3
   Lavadowas washed with water (2×50 ml)
4. 4
   Secadodried (MgSO4)
5. 5
   Otrothe solvents were evaporated in vacuo

Procedimiento

A mixture of 1-[1-(2-aminoethyl)-4-piperidyl]-3-(4-fluorophenyl)-5-methyl-1H-indole 12a (8.9 g), K2CO3 (4.2 g) and dichloromethane (80 ml) was cooled to 0°-5° C. and a solution of methyl chloroformate (2.9 g)in dichloromethane (50 ml) was added during 15 min. After reaction for further 2 h at room temperature the reaction mixture was washed with water (2×50 ml), dried (MgSO4) and the solvents were evaporated in vacuo. This afforded the 1-[1-(N-methoxycarbonyl-2-aminoethyl)-4piperidyl]-3-(4-fluorophenyl)-5-methyl-1H-indole, as an oil, which was used without further purification. Yield: 8.8 g.

Fuente