HCID 86671478, compound → HCID 68312636, compound

Participants

Reaction Steps

A solution of methanesulfonic acid 2-[2-(2-isopropyl-5-methyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-1,3a-diazabenzo[e]azulen-8-yloxy]-3-methanesulfonyloxy-2-methylpropyl ester (0.096 mmol) in benzylamine (0.5 mL) was heated at 150° C. for 1 h and then 180° C. for a further 1 h using microwave irradiation. After cooling to RT, the crude reaction mixture was purified by column chromatography (C18, gradient 15-55% MeOH in 0.5% TFA/H2O) and then loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH and the product eluted with 0.5M NH3/MeOH affording the title compound as a colourless gum (31 mg, 67% over two steps). LCMS (Method B): RT 2.40 min [M+H]+ 485

Provenance & Evidence