反应详情

5.5 g (11.3 mmol) of benzyl 4-[4-[(2S)-2-(t-butoxycarbonylamino)-3-hydroxypropyl]phenoxy]piperidine-1-carboxylate was dissolved in 60 ml of dichloromethane. 3.2 ml (22.6 mmol) of triethylamine and 1.95 g (17.0 mmol) of methanesulfonyl chloride were added to the solution. After stirring for 4 hours, the reaction mixture was treated by the isolation process with dichloromethane as the extractant in the same manner as that of step 1 in Example 1 to obtain an oily residue, which was dissolved in 120 ml of dimethylformamide. 2.57 g (60.6 mmol) of lithium chloride was added to the solution, and they were stirred at 50° C. for 15 hours. After the isolation process with ethyl acetate as the extractant in the same manner as that of step 1 in Example 1, the crude product was obtained, which was purified by the silica gel column chromatography to obtain the title compound.

1. customto obtain an oily residue, which
2. stirringwere stirred at 50° C. for 15 hours
3. customwhich was purified by the silica gel column chromatography