تفاعل #470981

معادلة التفاعل

2,4-dichloro-6-methylpyrimidine

1H-pyrazol-5-amine

NaI

DIEA

→

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

المردود 78.7%

المذيبات

NMP

EtOAc

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةthe mixture was cooled to room temperature
2. 2
   ترشيحThe precipitate was collected by filtration
3. 3
   غسيلwashed with the mixed solvent of hexane and EtOAc
4. 4
   أخرىdried in vacuo

الإجراء التجريبي

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.

المصدر