反应详情

2-(8-Methoxy-2-methylquinolin-4-ylamino)-2-phenylacetamide (example 74, 430 mg, 1.33 mmole) was suspended in tetrahydrofurane (20 mL) and BH3xSMe2 (2M in tetrahydrofurane) was added dropwise. The mixture was refluxed under stirring for 1 h and then stirred at RT for 12 hrs. The content of the flask was carefully mixed with 2N HCl and refluxed for 2 hrs. The reaction mixture was alkalized and extracted with dichloromethane. The organic phases were dried and concentrated. The residue thus obtained was purified using HPLC (RP-18, eluting with water/acetonitrile) to obtain the product (12%, 83 mg). ESI-MS [M+H]+=294.1 calculated for C22H21F6N3O5=293 g/mole

1. temperatureThe mixture was refluxed
2. stirringstirred at RT for 12 hrs
3. temperaturerefluxed for 2 hrs
4. extractionextracted with dichloromethane
5. customThe organic phases were dried
6. concentrationconcentrated
7. customThe residue thus obtained
8. customwas purified
9. washHPLC (RP-18, eluting with water/acetonitrile)