Réaction #42853

Équation de réaction

2,4,6-trifluoro-5-chloropyrimidine

3,5-dimethylpiperidine

→

5-chloro-2,4-difluoro-6-(3,5-dimethylpiperidino)pyrimidine

Solvants

tetrahydrofuran

Conditions de réaction

Traitement

1. 1
   Autrehalf hour

Mode opératoire

Into 6 ml of tetrahydrofuran solution of 0.5 g of 2,4,6-trifluoro-5-chloropyrimidine was added dropwise 0.34 g or 3,5-dimethylpiperidine (cis/trans diastereomer=about 4/1) at room temperature, and the mixture was stirred for one-and-half hour at same temperature. The reaction mixture was subjected to silica gel column chromatography to obtain 0.56 g of 5-chloro-2,4-difluoro-6-(3,5-dimethylpiperidino)pyrimidine. This compound had the cis/trans diastereomer originated two ethyls on the pyperidine ring. The ratio of the cis/trans diastereomer was about 5/1.

Source