Dimethyl Sulfoxide → HCID 11998030, compound

Participants

Reaction Steps

The title compound was prepared according to the procedure of Example 2 starting from 2,2,2-trichloro-1-{10-[(2′-methoxy-1,1′-biphenyl-4-yl)carbonyl]-10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl}ethanone of Example 1 (1.483 g, 2.75 mmole), (5-methyl-3-isoxazoyl)methylamine (0.256 g 1.0 eq), dimethylsulfoxide (5.0 eq, 0.896 g, 11.45 mmole), and triethylamine (2.2 eq, 0.510 g, 5 mmole) in 20 mL of acetonitrile. The residue was absorbed on silica gel Merck-60 and flash chromatographed using a gradient from 0 to 20% of ethyl acetate in dichloromethane, to provide a foam (0.460 g) which yielded an off-white solid upon treatment with ethyl acetate/hexane, m.p. 111-113° C.

Provenance & Evidence