Triphosgene → HCID 58902371, compound

Participants

Reaction Conditions

Reaction Steps

A solution of triphosgene (304 mg, 1.02 mmol) in THF (15 mL) was cooled to 0° C. To this solution was added TEA (0.74 mL, 5.32 mmol). A solution of 7-[(2-aminopyridin-4-yl)oxy]-N-(3-tert-butylphenyl)-1,2,3,4-tetrahydronaphthalene-2-carboxamide (850 mg, 2.04 mmol) in THF (6 mL) was added dropwise to the reaction mixture over the 20 min. The reaction mixture was allowed to stir at 0° C. and then to warm to rt and stir for 1 h. The reaction mixture was filtered and the filtrate was evaporated. The residue was purified by column chromatography to give N-(3-tert-butylphenyl)-7-[(2-isocyanatopyridin-4-yl)oxy]-1,2,3,4-tetrahydronaphthalene-2-carboxamide (510 mg, 56%) as yellow solid. LCMS: (FA) ES+442.5.

Provenance & Evidence