反应详情

To a solution of 1-(4-chlorophenyl)cyclopropanecarboxylic acid (39.3 mg, 0.2 mmol) in dichloromethane (2 mL) was added thionyl chloride (43.8 μL, 0.6 mmol) followed by DMF (1 drop) and the reaction was stirred at room temperature for 30 minutes and then the solvent was removed. Toluene (˜1 mL) was added, mixed with the residue and then removed by evaporation. The residue was then dissolved in dichloromethane (1 mL) and a solution of 6′-methoxy-3,5′-dimethyl-2,3′-bipyridin-6-amine (46 mg, 0.2 mmol) and triethyl amine (83.6 μL, 0.60 mmol) in dichloromethane (1 mL) was added. The reaction was stirred at room temperature for 12 hors. The reaction was then concentrated. The residue was dissolved in DMSO and purified by reverse phase HPLC (10-99% acetonitrile/water) to yield 62 mg of the product. ESI-MS m/z calc. 407.1. found 408.2 (M+1)+. Retention time 2.07 minutes.

1. customthe solvent was removed
2. additionToluene (˜1 mL) was added
3. additionmixed with the residue
4. customremoved by evaporation
5. dissolutionThe residue was then dissolved in dichloromethane (1 mL)
6. stirringThe reaction was stirred at room temperature for 12 hors
7. concentrationThe reaction was then concentrated
8. dissolutionThe residue was dissolved in DMSO
9. custompurified by reverse phase HPLC (10-99% acetonitrile/water)