Trifluoroacetic acid → HCID 68312736, compound

Participants

Reaction Steps

To a solution of [2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-1,3a-diazabenzo[e]azulen-9-yl]acetic acid tert-butyl ester (930 mg, 2.27 mmol) in DCM (20 mL) was added TFA (10 mL) and the resulting mixture stirred at RT for 1 h. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge which was washed with MeOH and the product eluted with 2M NH3/MeOH. The resulting residue was found to be acid and the corresponding methyl ester so was purified by column chromatography (Si-PCC, gradient 0-20% MeOH in DCM) affording [2-(2-Isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-1,3a-diazabenzo[e]azulen-9-yl]acetic acid as a white solid (164 mg, 21%). LCMS: RT 2.65 min [M+H]+ 354.3

Provenance & Evidence