Ethanol → HCID 86679716, compound

Participants

Reaction Conditions

Reaction Steps

(S)-6-(4-Chlorophenyl)-4-(2-(ethylamino)-2-oxoethyl)-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-8-yl trifluoromethanesulfonate (for a preparation see intermediate 3) (500 mg), 4-formylphenylboronic acid (166 mg), potassium carbonate (638 mg) and bis(triphenylphosphine)palladium(II) chloride (64.8 mg) were added to a 20 ml microwave vial. Ethanol (9 ml) and toluene (9 ml) were added to the vial. The reaction mixture was heated in a microwave at 120° C. for 20 min. The reaction mixture was filtered through Celite™ and the filter bed was washed with ethanol. The solvent was evaporated, and the residue was chromatographed (0-5% methanol:DCM) to give (S)-2-(6-(4-chlorophenyl)-8-(4-formylphenyl)-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide (327 mg) as a brown solid. LCMS (formate): MH+ 498/500, RT 0.98 min

Provenance & Evidence