反应详情

To a stirred solution of {(S)-1-[(S)-1-(2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]-3-methylpiperidin-3-yl}methanol (0.516 g, 1.8 mmol) in toluene (4 ml) was added tetrabutylammonium bromide (0.12 g) and 50% NaOH (4 ml). The mixture was stirred at RT for 15 min and bromoacetic acid tert-butyl ester (0.53 g) was added. After vigorous stirring at RT overnight, the reaction was quenched by addition of brine (15 ml) and the aqueous phase extracted twice with toluene. The combined organic phases were extracted with 1 M HCl solution and the acidic water phase was basified by addition of NaOH. Extraction with toluene and evaporation afforded the title compound (0.48 g) as an oil.

1. stirringAfter vigorous stirring at RT overnight
2. customthe reaction was quenched by addition of brine (15 ml)
3. extractionthe aqueous phase extracted twice with toluene
4. extractionThe combined organic phases were extracted with 1 M HCl solution
5. additionthe acidic water phase was basified by addition of NaOH
6. extractionExtraction
7. customwith toluene and evaporation