تفاعل #470982

معادلة التفاعل

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

المردود 42.2%

المذيبات

DMF

ظروف التفاعل

المعالجة

1. 1
   تركيزThe mixture was concentrated
2. 2
   أخرىto remove DMF
3. 3
   ترشيحThe insoluble material was filtered off
4. 4
   غسيلwashed with EtOAc
5. 5
   تركيزThe filtrate was concentrated

الإجراء التجريبي

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.

المصدر