反应详情

A solution of (R)-toluene-4-sulfonic acid 2-(tert-butyl-dimethyl-silanyloxy)-2-(6-chloro-pyridin-3-yl)-ethyl ester (12.0 g) and 11.4 g of 2-amino-2-methyl-1-(4-nitrophenyl)propane (prepared by the method described in J. Milecki, et al. J. Med. Chem., 30, 1563 (1987)) in DMSO (30 mL) was stirred at 100° C. for 48 h. The reaction solution was partitioned between ethyl ether/water, the resulting organic layer washed with water (3×), brine, dried over sodium sulfate and concentrated in vacuo to afford an oil. Flash chromatography on silica gel (20% to 50% ethyl acetate/hexanes) afforded 8.0 g of the title compound (I-2f) as a golden oil.

1. customThe reaction solution was partitioned between ethyl ether/water
2. washthe resulting organic layer washed with water (3×), brine
3. dry with materialdried over sodium sulfate
4. concentrationconcentrated in vacuo
5. customto afford an oil