Hydrochloric Acid → HCID 68522948, compound

Participants

Reaction Steps

4-(3-chloro-2-fluoroanilino)-6-[(3R)-1-(tert-butoxycarbonyl)pyrrolidin-3-yloxy]-7-methoxyquinazoline (2.3 g, 4.7 mmole) was dissolved in acetonitrile (35 ml) and hydrogen chloride (4.0M in 1,4-dioxane) (4.7 ml, 18.8 mmole) was added. The mixture was heated to reflux for one hour. After cooling to room temperature, the solid was filtered, washed with acetonitrile and diethylether, and dried under vacuum to give 4-(3-chloro-2-fluoroanilino)-6-[(3R)-pyrrolidin-3-yloxy]-7-methoxyquinazoline hydrochloride as a white solid (1.9 g, 95%); 1H NMR Spectrum (DMSO d6) 2.17-2.29 (m, 1H); 2.34-2.44 (m, 1H); (m, 3H); 3.72-3.84 (m, 1H); 4.00 (s, 3H); 5.44 (m, 1H); 7.31-7.38 (m, 1H); 7.45 (s, 1H); 7.49-7.55 (m, 1H); 7.59-7.65 (m, 1H); 8.67 (s, 1H); 8.80 (s, 1H); 9.43 (br.s 1H); 9.62 (br.s, 1H); 12.25 (br.s, 1H); Mass Spectrum: (M−H)− 387.

Provenance & Evidence