反应详情

4-(2-Methoxy-ethyl)-piperidine-4-carboxylic acid ethyl ester (1 g) was dissolved in pyridine (15 ml) under an argon atmosphere at RT and 2-methyl-propane-1-sulfonyl chloride (0.728 g) was added and the mixture was stirred for 60 h at RT. The pyridine was evaporated off, the residue dissolved in AcOEt, washed with 0.05M HCl and brine. The layers were separated, the organic layer dried over sodium sulphate and concentrated. The crude product was purified by flash chromatography (AcOEt/heptane, gradient from 0 to 25%,) to give the desired 4-(2-methoxy-ethyl)-1-(2-methyl-propane-1-sulfonyl)-piperidine-4-carboxylic acid ethyl ester (0.63 g) as a yellow oil. MS (ESI): 336.18 (MH+).

1. customThe pyridine was evaporated off
2. dissolutionthe residue dissolved in AcOEt
3. washwashed with 0.05M HCl and brine
4. customThe layers were separated
5. dry with materialthe organic layer dried over sodium sulphate
6. concentrationconcentrated
7. customThe crude product was purified by flash chromatography (AcOEt/heptane, gradient from 0 to 25%,)