Reacción #78345

Ecuación de reacción

hydrogen chloride

4-benzyl-4-(pyrrolidin-1-ylcarbonyl)piperidine p-toluene-sulfonate

compound

1-Benzoyl-3-(3,4-dichlorophenyl)-3-[3-[4-(pyrrolidin-1-ylcarbonyl)piperid-1-yl]propyl]piperidine Hydrochloride

K2CO3

→

expected product

1-Benzoyl-3-[3-[4-benzyl-4-(pyrrolidin-1-ylcarbonyl)piperid-1-yl]propyl]-3-(3,4-dichlorophenyl)piperidine Hydrochloride Hemihydrate

Disolventes

water

DMF

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrothe precipitate formed
2. 2
   Filtraciónis filtered off
3. 3
   Lavadowashed with water
4. 4
   workup.DISSOLUTIONThe precipitate is dissolved in AcOEt
5. 5
   Secadothe organic phase is dried over MgSO4
6. 6
   Otrothe solvent is evaporated off under vacuum
7. 7
   OtroThe residue is chromatographed on silica H
8. 8
   OtroThe product obtained
9. 9
   Otrothe precipitate formed
10. 10
    Filtraciónis filtered off

Procedimiento

A mixture of 4-benzyl-4-(pyrrolidin-1-ylcarbonyl)piperidine p-toluene-sulfonate, 0.65 g of the compound obtained in step B of EXAMPLE 1 and 0.7 g of K2CO3 in 6 ml of DMF is heated at 80° C. for 3 hours. The reaction mixture is poured into iced water and the precipitate formed is filtered off and washed with water. The precipitate is dissolved in AcOEt, the organic phase is dried over MgSO4 and the solvent is evaporated off under vacuum. The residue is chromatographed on silica H using DCM and then a DCM/MeOH mixture (95/5; v/v) as the eluent. The product obtained is taken up with ethereal hydrogen chloride and the precipitate formed is filtered off to give 0.56 g of the expected product.

Fuente