HCID 86671480, compound → HCID 68313039, compound

Participants

Reaction Steps

A solution of methanesulfonic acid 2-cyclopropylmethyl-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-methanesulfonyloxypropyl ester from Example 283 (90 mg, 0.1476 mmol) in benzylamine (1 mL) was heated at 180° C. for 2.5 h using microwave irradiation. After cooling to RT, the crude reaction mixture was purified by column chromatography (C18, gradient 30-65% 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 (65 mg, 84%). LCMS (Method B): RT 2.66 min [M+H]+ 525

Provenance & Evidence