Reacción #551997

Ecuación de reacción

N,N-dimethylformamide

3-aminoindazole

1-(2-bromoethyl)piperidine hydrobromide

potassium carbonate

→

3-(2-piperidinoethylamino)indazole

Rendimiento 56.0%

Disolventes

water

chloroform

chloroform

Condiciones de reacción

Tratamiento posterior

1. 1
   workup.ADDITIONwere mixed
2. 2
   workup.ADDITIONwere added to the condensed residue
3. 3
   OtroThen the chloroform layer was separated
4. 4
   Secadodried with anhydrous sodium sulate and chloroform
5. 5
   Otrowas removed under reduced pressure
6. 6
   OtroThe residue thus obtained

Procedimiento

4.0 g of 3-aminoindazole prepared by the method described in C. E. KWARTLER et. al., J. Am. Chem. Soc., 65, 1804 (1943), 8.18 g of 1-(2-bromoethyl)piperidine hydrobromide obtained from Referential Example 1, 8.28 g of anhydrous potassium carbonate and 80 ml of dried N,N-dimethylformamide were mixed and stirred for 24 hours at 80° C. After the reaction mixture was condensed under reduced pressure, 100 ml of chloroform and 50 ml of water were added to the condensed residue. Then the chloroform layer was separated, dried with anhydrous sodium sulate and chloroform was removed under reduced pressure. The residue thus obtained was subjected to alumina-column chromatography (alumina: 200 g) using chloroform as the solvent to give 4.09 g of 3-(2-piperidinoethylamino)indazole in a yield of 56%.

Fuente