Hydrochloric Acid → N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-7-[(2E)-4-(dimethylamino)but-2-enoyl]-5,6,7,8-tetrahydropyrido[4',3':4,5]furo[2,3-d]pyrimidin-4-amine

Participants

Reaction Conditions

Reaction Steps

tert-Butyl 4-({3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}amino)-5,8-dihydropyrido[4′,3′:4,5]furo-[2,3-d]pyrimidine-7(6H)-carboxylate from Example 86A (18 mg, 0.034 mmol) was dissolved in 2-propanol (1.0 mL) and treated with 4 M gaseous hydrogen chloride in dioxane (0.25 mL, 1.0 mmol). The mixture was heated to 80° C. for 2 h. Subsequently, the solvent was removed in vacuo. The residue was reacted in analogy to Example 89 with (2E)-4-(dimethylamino)but-2-enoic acid hydrochloride from Example 1A (8.0 mg, 0.048 mmol) to yield 7.0 mg (38%) of the title compound.

Provenance & Evidence