反应详情

1 g of the product obtained in Step 1 (containing 46% amidine) is dissolved in 15 mL of methanol and then 86 mg (2.26 mmol, 1.2 equivalents) of sodium tetraborohydride are added at ambient temperature. Stirring is carried out overnight at ambient temperature, and then 5 mL of 20% aqueous sodium hydroxide solution and 20 mL of dichloromethane are added. Vigorous stirring is carried out for 15 minutes. The organic phase is then extracted, washed with water, dried over MgSO4, filtered and then evaporated to dryness. There is obtained 1 g of an oil which is purified by flash chromatography on 100 g of silica (eluant=dichloromethane/ethanol/NH4OH: 90/10/1) to yield 210 mg of the title product in the form of an oil.

1. stirringVigorous stirring
2. waitis carried out for 15 minutes
3. extractionThe organic phase is then extracted
4. washwashed with water
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. customevaporated to dryness