2-Fluoro-5-methylphenyl isocyanate → HCID 118130070, compound

Participants

Reaction Steps

A solution of methyl 5-[N-({6-amino-5-[(3-aminophenyl)ethynyl]pyridin-3-yl}carbonyl)-S-methylsulfonimidoyl]pentanoate (85.6 mg, 0.2 mmol, 1 eq) and 2-fluoro-5-methylphenyl isocyanate (29 μL, 1.1 eq) in anhydrous DMF (2 mL) was stirred at room temperature overnight. The reaction was then diluted with EtOAc, washed sequentially with aq NH4Cl, saturated aq NaHCO3, brine, and lastly dried with sodium sulfate. The clear solution was decanted, concentrated, and the oily residue was subject to a gradient column chromatography (EtOAc-Hex from 1:1 to neat EtOAc). The product containing fractions were concentrated to give the title compound as a white foam (86.2 mg).

Provenance & Evidence