反应详情

To a solution of tert-butyl 6-(hydroxymethyl)pyridin-2-ylcarbamate 78 (3.0 g, 13.4 mmol) and diisopropylethylamine (5.0 g, 40 mmol) in acetonitrile (30 mL) was added methanesulfonyl chloride (2.0 g, 17.4 mmol) over a period of 30 min at 0° C. and the mixture was stirred for 2 h at room temperature. The reaction was quenched by adding saturated aqueous NaHCO3 and extracted with ethyl acetate (3×60 mL). The combined organic layers were washed with brine, dried (Na2SO4) and concentrated under reduced pressure to afford quantitative yield of crude 79.

1. customThe reaction was quenched
2. additionby adding saturated aqueous NaHCO3
3. extractionextracted with ethyl acetate (3×60 mL)
4. washThe combined organic layers were washed with brine
5. dry with materialdried (Na2SO4)
6. concentrationconcentrated under reduced pressure
7. customto afford quantitative yield of crude 79