Dimethyl Sulfoxide → N-[(1-Methyl-1H-pyrrol-2-yl)methyl]-10-[(2,2',6'-trimethyl-1,1'-biphenyl-4-yl)carbonyl]-10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-3-carboxamide

Participants

Reaction Steps

The title compound was prepared according to procedure of Example 2 starting from 2,2,2-trichloro-1-{10-[(2,2′,6′-trimethyl-1,1′-biphenyl-4-yl)carbonyl]-10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl}ethanone of Example 3 (1.4 g, 2.5 mmole), (1-methyl-1H-pyrrol-2-yl)methylamine (0.234 g, 2.1 mmole), dimethylsulfoxide (0.822 g, 10.5 mmole) and triethyl amine (0.470 g, 4.6 mmole) in 15 mL of acetonitrile, Flash chromatography of the residue on silica gel Merck-60 (0-25% ethyl acetate in dichloromethane) gave a foam (0.924 g) which solidified upon treatment with ethyl acetate/hexane/dichloromethane, mp. 222-224° C.

Provenance & Evidence