Reaktion #470981

Reaktionsgleichung

2,4-dichloro-6-methylpyrimidine

1H-pyrazol-5-amine

NaI

DIEA

→

2-chloro-6-methyl-N-(1H-pyrazol-5-yl)pyrimidin-4-amine

Ausbeute 78.7%

Lösungsmittel

NMP

EtOAc

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturthe mixture was cooled to room temperature
2. 2
   FiltrationThe precipitate was collected by filtration
3. 3
   Waschenwashed with the mixed solvent of hexane and EtOAc
4. 4
   Sonstigedried in vacuo

Vorschrift

To the solution of 2,4-dichloro-6-methylpyrimidine (3.00 g) and 1H-pyrazol-5-amine (1.31 g) in NMP (30 ml) was added NaI (2.36 g) and DIEA (6.33 ml). And the mixture was heated to 80° C. under stirring. After 1 day, the mixture was cooled to room temperature. The mixture was diluted with EtOAc. The precipitate was collected by filtration, washed with the mixed solvent of hexane and EtOAc and dried in vacuo to give 2-chloro-6-methyl-N-(1H-pyrazol-5-yl)pyrimidin-4-amine (2.60 g) as a pale pink solid.

Quelle