Hydrochloric Acid → HCID 86603906, compound

Participants

Reaction Steps

Hydrochloric acid (10.4 ml of a 4.0 N solution in 1,4-dioxane, 41.5 mmol) was added, dropwise to a solution of di(tert-butyl) ((2S)-1-(3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1,3-thiazol-2-yl)amino)-6-methoxyquinazolin-7-yl)oxy)propyl)pyrrolidin-2-yl)methyl phosphate (4.49 g, 5.92 mmol) in 1,4-dioxane (180 ml) upon which a light yellow solid precipitated from the reaction mixture. The resulting heterogeneous reaction mixture was stirred for a further 20 hours before the precipitate was collected, washed with 1,4-dioxane (80 ml) and acetonitrile (2×100 ml) and dried in vacuo to yield ((2S)-1-(3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1,3-thiazol-2-yl)amino)-6-methoxyquinazolin-7-yl)oxy)propyl)pyrrolidin-2-yl)methyl dihydrogen phosphate bis-hydrochloride as a light yellow solid (4.40 g, 97% yield):

Provenance & Evidence