反应详情

A solution of 4-[2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-1,3a-diazabenzo[e]azulene-9-sulfonyl]piperazine-1-carboxylic acid tert-butyl ester (175 mg, 0.32 mmol) in DCM (3 mL) was treated with TFA (3 mL) and the resulting mixture stirred at RT for 1 h then concentrated in vacuo. The resulting residues was loaded onto an Isolute® SCX-2 cartridge which was washed with MeOH and eluted with 2M NH3/MeOH affording 2-(2-Isopropyl-2H-[1,2,4]triazol-3-yl)-9-(piperazine-1-sulfonyl)-4,5-dihydro-6-oxa-1,3a-diazabenzo[e]azulene (126 mg, 88%). LCMS: RT 2.20 and 0.32 min [M+H]+ 444.3

1. concentrationthen concentrated in vacuo
2. washwas washed with MeOH
3. washeluted with 2M NH3/MeOH