(3-Trifluoromethylphenyl)urea → HCID 59684776, compound

Participants

Reaction Steps

A stirred mixture of benzyl 2-acetoacetylpiperidine-1-carboxylate (Example 10A) (1.74 g, 5.74 mmol), 4-cyanobenzaldehyde (752 mg, 5.74 mmol), N-[3-(trifluoromethyl)phenyl]urea (976 mg, 4.78 mmol) and 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane 2,4,6-trioxide anhydride (6.1 g, 9.5 mmol) in methyl tert.-butyl ether (44 ml) is refluxed overnight (16 h). The product is extracted with methyl tert.-butyl ether (300 ml), washed with aq. saturated sodium bicarbonate solution (200 ml), dried with anhydrous magnesium sulfate, filtered and concentrated. The residue is chromatographed with silica gel 60 using cyclohexane/ethyl acetate as eluent.

Provenance & Evidence