1-Hydroxybenzotriazole → HCID 18621203, compound

Participants

Reaction Steps

Carboxylic acid from Step M (1.02 g, 3.76 mmol), amine from Step F (1.80 g, 3.76 mmol), EDC hydrochloride (865 mg, 4.51 mmol), HOBT (610 mg, 4.51 mmol), and N,N-diisopropylethylamine (3.28 mL, 18.8 mmol) were stirred in dry DMF (20 mL) at 25° C. for 72 hours. The reaction was poured onto aq. NaHCO3 (100 mL) and extracted with methylene chloride (3×50 mL). The combined organic layers were dried (Na2SO4), filtered, and concentrated in vacuo. The crude product was purified by column chromatography (1→5% MeOH/CH2Cl2) to provide the title compound as a yellow oil.

Provenance & Evidence