反应详情

A solution of the 3-piperidin-3-yl-1H-indole obtained in Example 29 in acetone/water (1:1) at 0° C. is treated with di-tert-dicarbonate (4.1 g, 18.7 mmol) and K2CO3 (11.75 g, 85 mmol), stirred for 2 hours while warming to room temperature, and concentrated in vacuo. The resultant aqueous mixture is extracted with ethyl acetate. The extracts are combined, dried over Na2SO4 and concentrated in vacuo. The resultant residue is purified by column chromatography (silica gel, 1% NH4OH in MeOH:CHCl3, 0:100 to 10:90 as eluent) to afford the title product, 1.25 g, identified by HPLC and mass spectral analyses.

1. concentrationconcentrated in vacuo
2. extractionThe resultant aqueous mixture is extracted with ethyl acetate
3. dry with materialdried over Na2SO4
4. concentrationconcentrated in vacuo
5. customThe resultant residue is purified by column chromatography (silica gel, 1% NH4OH in MeOH:CHCl3, 0:100 to 10:90 as eluent)