Phosphorus oxychloride → 4,8-Dichloro-2-(4-isopropyl-thiazol-2-yl)-7-(2-morpholin-4-yl-ethoxy)-quinoline

Participants

Reaction Conditions

Reaction Steps

8-Chloro-2-(4-isopropyl-thiazol-2-yl)-7-(2-morpholin-4-yl-ethoxy)-quinolin-4-ol (5.0 g, 11.5 mmol) in dioxane (50 mL) were stirred at room temperature. POCl3 (5.4 g, 34.6 mmol) was added slowly to the reaction mixture. The reaction was heated to 85° C. with stirring for 10 mins. The reaction was cooled to room temperature and was quenched with ice water. The solution was extracted with ethyl acetate (3×100 mL). The combined organics were dried with sodium sulfate, filtered and were concentrated. Compound XX (4.6 g, 90%) was purified by silica gel chromatography.

Provenance & Evidence