反应详情

Morpholine (0.05 ml, 0.54 mmol) and acetic acid (0.03 ml, 0.54 mmol) were added to solution of 2-([(3,4-difluorophenyl)methyl]oxy)-5-formyl-N-3-pyridinylbenzamide (may be prepared by Example 80; 200 mg, 0.54 mmol) in DCE (5 ml), and the mixture was stirred at room temperature for 10 min. Sodium triacetoxyborohydride (173 mg, 0.81 mmol) was then added and the mixture was warmed to 50° C. overnight. Saturated sodium hydrogencarbonate (10 ml) was added and the mixture stirred for 10 min before being diluted with dichloromethane (25 ml). The organic layer was separated and the aqueous phase was extracted with dichloromethane (25 ml), the organic were combined and evaporated under reduced pressure. The residue was purified by MDAP to yield the title compound. 82 mg.

1. temperaturethe mixture was warmed to 50° C. overnight
2. stirringthe mixture stirred for 10 min
3. customThe organic layer was separated
4. extractionthe aqueous phase was extracted with dichloromethane (25 ml)
5. customevaporated under reduced pressure
6. customThe residue was purified by MDAP