反应详情

A solution of 2-{[(3,4-difluorophenyl)methyl]oxy}-5-formyl-N-3-pyridinylbenzamide (may be prepared as described in Example 80; 100 mg, 0.27 mmol) in tetrahydrofuran (5 ml) was cooled to 0° C. and methylmagnesium bromide (0.18 ml, 0.54 mmol) was added. The mixture was allowed to warm to room temperature and stirred overnight. An additional 3 eq of methylmagnesium bromide was added and the mixture was stirred at room temperature. 5 ml of 1M aqueous sulphuric acid was then added. After stirring for 30 min the mixture was extracted with ethyl acetate (3×10 ml). The organics were combined, evaporated under reduced pressure and the residue was purified by MDAP to yield the title compound. 48 mg.

1. stirringthe mixture was stirred at room temperature
2. stirringAfter stirring for 30 min the mixture
3. extractionwas extracted with ethyl acetate (3×10 ml)
4. customevaporated under reduced pressure
5. customthe residue was purified by MDAP