反应详情

A solution of the 1′-[(6-chloro-1H-indol-3-yl)carbonyl]-3H-spiro[2-benzofuran-1,4′-piperidine] (prepared according to example 69) in dry DMF was treated with NaH (1.1 eq) and stirred for 10 min at room temperature, then treated with (S)-3-methanesulfonyloxymethyl-piperidine-1-carboxylic acid tert-butyl ester (1.1 eq) (JP 2001278872) and stirred at room temperature for 16 h then 70° for 4 h. Concentration and treatment with excess HCl in dioxane gave after purification by preparative HPLC the desired product in 39% yield.

1. stirringstirred at room temperature for 16 h
2. wait70° for 4 h
3. concentrationConcentration and treatment with excess HCl in dioxane
4. customgave
5. customafter purification by preparative HPLC the desired product in 39% yield