Reaktion #470982

Reaktionsgleichung

2,4-dichloro-6-methylpyrimidine

3-cyclopropyl-1H-pyrazol-5-amine

NaI

DIEA

→

2-chloro-N-(3-cyclopropyl-1H-pyrazol-5-yl)-6-methylpyrimidin-4-amine

Ausbeute 42.2%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   EinengenThe mixture was concentrated
2. 2
   Sonstigeto remove DMF
3. 3
   FiltrationThe insoluble material was filtered off
4. 4
   Waschenwashed with EtOAc
5. 5
   EinengenThe filtrate was concentrated

Vorschrift

To the solution of 2,4-dichloro-6-methylpyrimidine (1.63 g) and 3-cyclopropyl-1H-pyrazol-5-amine (1.24 g) in DMF (20 ml) was added NaI (1.49 g) and DIEA (1.72 ml). And the mixture was stirred at 80° C. overnight. The mixture was concentrated to remove DMF. The residue was suspended into EtOAc. The insoluble material was filtered off and washed with EtOAc. The filtrate was concentrated and the residue was pufiried with silica gel column chromatography (eluent: CHCl3/MeOH=98/2˜90/10) to give 2-chloro-N-(3-cyclopropyl-1H-pyrazol-5-yl)-6-methylpyrimidin-4-amine (1054 mg) as a pale pink solid.

Quelle