反应详情

A solution of N-cyclopropyl-3-(1H-indazol-5-yl)-4-methylbenzamide (Example 17) (0.07 g) in dry DMF (3 ml) was treated with sodium hydride (60% oil dispersion, 0.014 g) under nitrogen. After 5 min 1,1-dimethylethyl 4-[(methylsulfonyl)oxy]-1-piperidinecarboxylate (0.08 g) was added and the mixture was stirred at room temp. for 18 h. 0.88 Ammonia (1 ml) was added and the mixture was concentrated under vacuum. The residue was purified by column chromatography on silica eluting with cyclohexane:ethyl acetate (1:1) followed by reverse phase preparative Hplc to give the title compound (0.005 g).

1. concentrationthe mixture was concentrated under vacuum
2. customThe residue was purified by column chromatography on silica eluting with cyclohexane:ethyl acetate (1:1)