반응 #2469283

반응 방정식

3-methyl-pyrrolo[2,3-c]pyridin-1-yl amine

4-methyl-2-pyridin-2-yl-pyrimidine-5-carboxylic acid

HATU

DIPEA

NaHCO3

→

4-methyl-2-pyridin-2-yl-pyrimidine-5-carboxylic acid (3-methyl-pyrrolo[2,3-c]pyridin-1-yl)-amide

수율 44.2%

용매

DMF

water

반응 조건

후처리

1. 1
   workup.ADDITIONare added
2. 2
   여과The resulting solid is collected by filtration
3. 3
   기타triturated with hot water
4. 4
   여과The mixture is filtered again
5. 5
   기타the solid is dried under vacuum

실험 절차

A mixture of 3-methyl-pyrrolo[2,3-c]pyridin-1-yl amine (467 mg, 3.18 mmol), 4-methyl-2-pyridin-2-yl-pyrimidine-5-carboxylic acid (683 g, 3.18 mmol), HATU (1.45 g, 3.81 mmol), DIPEA (1.23 g 9.54 mmol) in DMF (10 mL) is stirred at 1500 C. for 1 h. The reaction is quenched with water, and NaHCO3 (320 mg, 3.81 mmol) and EtOAC are added. The resulting solid is collected by filtration and then triturated with hot water. The mixture is filtered again and the solid is dried under vacuum to afford 4-methyl-2-pyridin-2-yl-pyrimidine-5-carboxylic acid (3-methyl-pyrrolo[2,3-c]pyridin-1-yl)-amide (484 mg). MS: 345 (M+H); 1H NMR (300 MHz, CD3OD): δ 9.24 (s, 1H), 8.79 (d, 2H), 8.65 (d, 1H), 8.21 (d, 1H), 8.05 (t, 1H), 7.72 (d, 1H), 7.60 (s, 1H), 7.57 (s, 1H), 2.88 (s, 3H), 2.40 (s, 3H).

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