Trimethylsilyldiazomethane → HCID 68828891, compound

Participants

Reaction Steps

(Trimethylsilyl)diazomethane (8.1 mL, 2M in THF, 16.2 mmol) was added to a solution of 3-bromo-5-(2-fluoro-phenylamino)-isonicotinic acid (4.2 g, 13.5 mmol) in THF/MeOH (72 mL, 9/1, v/v) and stirred for 2 h at room temperature. The reaction solution was quenched with acetic acid, and then concentrated. The crude product was purified via Biotage eluting with a gradient of 0 to 50% EtOAc in hexanes to afford the desired product (4.1 g, 94%) as a yellow solid.

Provenance & Evidence