反应详情

温度

80 °C

N-[2-(cyanomethyl)-4′-methyl-4,5′-bi-1,3-thiazol-2′-yl]acetamide, Compound (3) (50 mg; 0.18 mmol; 1 eq.), is dissolved in dioxane (10 ml). Hydroxylamine hydrochloride (15 mg; 0.22 mmol; 1.20 eq.) and N,N-diethylethanamine (0.03 ml; 0.22 mmol; 1.20 eq.) are added and reaction mixture is heated at 80° C. overnight. Reaction mixture is cooled down and dioxane evaporated. The residue is taken up in EtOAc and washed several times with water (3×10 mL). The organic phases are dried over MgSO4, filtrated and evaporated. Crude material is purified by flash chromatography on silica gel (cyclohexane/ethylacetate, 50/50), affording the title compound as an oil (50 mg; 95%).

1. customreaction mixture
2. customReaction mixture
3. temperatureis cooled down
4. customdioxane evaporated
5. washwashed several times with water (3×10 mL)
6. dry with materialThe organic phases are dried over MgSO4
7. filtrationfiltrated
8. customevaporated
9. customCrude material is purified by flash chromatography on silica gel (cyclohexane/ethylacetate, 50/50)