Diisopropylethylamine → 1-(2-Chloro-4-cyano-phenyl)-3-(2-hydroxymethyl-indan-2-yl)-urea

Participants

Reaction Steps

To a mixture of 2-chloro-4-cyano-aniline (150 mg) and N,N-diisopropylethylamine (0.34 ml) in THF (15 ml), a solution of triphosgene (96 mg) in THF (5 ml) was added dropwise at room temperature. The mixture was stirred at room temperature for 30 min. To the mixture, a solution of 2-amino-2,3-dihydro-1H-indene-2-methanol (160 mg, WO 9110644) in THF (2 ml) was added at room temperature. The mixture was stirred for 1 hr at room temperature. The mixture was diluted with AcOEt, washed with water and brine, dried over MgSO4 and evaporated. The residue was triturated with CH2Cl2 to obtain the title compound (270 mg, 80%) as a white solid.

Provenance & Evidence