反应详情

A solution of 1-(4-(2-(cis-3-(benzo[d]thiazol-2-ylamino)cyclobutoxy)pyridin-3-yl)-5,6-dihydropyridin-1(2H)-yl)ethanone (0.12 g, 0.28 mmol) in ethanol (2 mL) was added palladium hydroxide, 20 wt. % Pd (dry basis) on carbon, wet, Degussa type E101 NE/W (0.039 g, 0.056 mmol) and hydrogenated (double-walled balloon pressure) at 50° C. for 3 days. The cooled reaction was filtered via a pad of Celite®, and the filtrate was concentrated in vacuo and purified via flash column chromatography (20% EtOAc/Hexanes to 100% EtOAc) to afford 1-(4-(2-(cis-3-(benzo[d]thiazol-2-ylamino)cyclobutoxy)pyridin-3-yl)piperidin-1-yl)ethanone as a white solid. [M+1]=423.0. IC50 (uM): 0.001566.

1. customThe cooled reaction
2. filtrationwas filtered via a pad of Celite®
3. concentrationthe filtrate was concentrated in vacuo
4. custompurified via flash column chromatography (20% EtOAc/Hexanes to 100% EtOAc)