Triethylamine → 1-[[2,3,4,5-Tetrahydro-3-[[1-[(2-methyl-5-benzofuranyl)amino]-2-nitroethenyl]amino]-2-oxo-1H-1-benzazepin-1-yl]acetyl]pyrrolidine

Participants

Reaction Conditions

Reaction Steps

A solution of 2-methyl-5-benzofuranamine (0.24 mmol), 1,1-bis(methylthio)-2-nitroethylene (40 mg, 0.24 mmol) and triethylamine (0.035 mL, 0.25 mmol) in ethanol (0.35 mL) was stirred at 80° C. for 2 h. To the mixture was added 1-[(3-amino-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-1-yl)acetyl]pyrrolidine (70 mg, 0.24 mmol) and the resulting reaction was stirred at 80° C. overnight. The reaction mixture was purified by column chromatography (silica, 3% methanol/ethyl acetate) to provide the title compound (29 mg, 24% yield): MS (ESI, pos. ion spectrum) m/z 504; HPLC (method A) tR 3.67 min.

Provenance & Evidence