反应详情

2-nitro-4-(1-piperidin-4-ylmethoxy)5-methoxybenzonitrile (771 mg, 2.65 mmol) in CH2Cl2 (8 ml) and MeOH (4 ml) was reacted for 0.5 hour with formaldehyde (13.3 M, 300 μl, 4 mmol), acetic acid (191 mg, 3.18 mmol) and NaBH(OAc)3 (674 mg, 3.18 mmol) slowly added over 15 minutes. The solution was evaporated, the oily residue was taken up in a mixture of Na2CO3 and ethylacetate, extracted with ethylacetate. The organic phase was dried over MgSO4, evaporated to give title compound as a yellow solid (698 mg, 86%).

1. additionslowly added over 15 minutes
2. customThe solution was evaporated
3. additionthe oily residue was taken up in a mixture of Na2CO3 and ethylacetate
4. extractionextracted with ethylacetate
5. dry with materialThe organic phase was dried over MgSO4
6. customevaporated