1H-1,2,4-Triazole → (4S)-11-[2-(dimethyl-[1,2,4]triazol-1-ylmethylsilanyl)-ethyl]-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione

Participants

Reaction Steps

A solution of Compound 4 (60 mg), 1,2,4-triazole (22 mg) and NaHCO3 (26 mg) in dry N,N-dimethylformamide (1 mL) was heated at 70° C. for 5 hours under argon. The N,N-dimethylformamide was removed from the reaction mixture under vacuum and the residue was directly eluted on a silica gel column using 4% ethanol in dichloromethane to obtain the required product in 79% yield (43 mg).

Provenance & Evidence