HCID 67496496, compound → HCID 86664836, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-difluoro-2-(3-nitro-5-(pyridin-4-yl)phenyl)acetic acid 52.D (450 mg, 1.53 mmol) in toluene (5 mL) was added n,n-dimethylformamide di-tert-butyl acetal (1.47 mL, 6.12 mmol). The mixture was stirred at 50° C. for 1 hour, then concentrated and dried under vacuum. The residue was then dissolved in EtOAc (10 mL), to which was added 10% Pd/C (150 mg). The air was then evacuated out of the flask and replaced by hydrogen. The mixture was stirred at room temperature for 2 hours, filtered over celite and then concentrated to afford tert-butyl 2-(3-amino-5-(pyridin-4-yl)phenyl)-2,2-difluoroacetate 52.E (473 mg, 96% yield) which is used in the next step with no further purification.

Provenance & Evidence