Water → HCID 86694779, compound

Participants

Reaction Steps

At −15° C., 51 μl (0.70 mmol) of chlorosulphonyl isocyanate were added slowly to a solution of 160 mg (0.50 mmol) of (2S)-tert-butyl {1-hydroxy-3-[3-(trifluoromethyl)phenyl]propan-2-yl}carbamate (for the preparation see US patent application 2008/0242694, Example [0464]) in 7.6 ml of acetonitrile. The reaction mixture was stirred at RT for 1 h, 1 ml of water was then added and the mixture was heated at 60° C. overnight. An analytical sample showed complete conversion into the target product according to LC/MS. After cooling to RT, the volatile components were removed on a rotary evaporator and finally under high vacuum. The residue (80 mg, 53% of theory) corresponded to the title compound.

Provenance & Evidence