Methanol → HCID 67282314, compound

Participants

Reaction Steps

5-(4-Aminopiperidin-1-yl)-7-chloro-1-methyl-3-(naphthalen-2-ylmethyl)-1H-benzo[e][1,4]diazepin-2(3H)-one (50 mg, 0.11 mmol) was dissolved in dichloromethane (0.5 mL) and triethylamine (31 μL, 0.22 mmol), acetic anhydride (11 μL, 0.11 mmol) was added and the mixture was stirred at ambient temperature for 1 hour. To the solution was added silica and concentrated in vacuo. Column chromatography eluting with a gradient of 70-100% ethyl acetate in hexanes then 0-15% methanol in ethyl acetate provided N-(1-(7-chloro-1-methyl-3-(naphthalen-2-ylmethyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-5-yl)piperidin-4-yl)acetamide (30 mg, 55% yield). ESI m/z measured 489.2043 [M+H]+. calculated 489.2057.

Provenance & Evidence