反应 #166796

反应方程式

5-Bromo-4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-amine

Na2CO3

BOP-Cl

Triethylamine

nicotinic acid

→

N-(5-bromo-4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)nicotinamide

收率 55.0%

溶剂

DMF

LiOH

反应条件

后处理

1. 1
   workup.STIRRINGstirred for 10 minutes
2. 2
   萃取extracted into DCM
3. 3
   其他dried
4. 4
   过滤filtered
5. 5
   浓缩concentrated
6. 6
   其他to give a crude residue
7. 7
   其他The crude residue was triturated with 1:2 MeOH/DCM

实验过程

5-Bromo-4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-amine (0.044 g, 0.19 mmol), nicotinic acid (0.0283 g, 0.230 mmol), and BOP-Cl (0.0584 g, 0.230 mmol) were placed in DMF (3 mL) at room temperature. Triethylamine (0.133 mL, 0.956 mmol) was then added, and the reaction was stirred for 1 hour at room temperature. The reaction was then diluted with 3M LiOH (aq., 0.5 mL) and stirred for 10 minutes. The reaction was then poured into saturated Na2CO3, extracted into DCM, and the organic fractions were combined, dried, filtered and concentrated to give a crude residue. The crude residue was triturated with 1:2 MeOH/DCM to give N-(5-bromo-4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)nicotinamide (0.035 g, 54.6% yield) as a solid.

来源