Ammonia → HCID 66734869, compound

Participants

Reaction Steps

Under an atmosphere of argon protective gas, a 0.5 M solution of ammonia in dioxane (4000 μl, 2021 μmol; 10 eq.) and triethylamine (20.4 mg, 202 μmol; 1 eq.) were added to 5-cyano-2-{(4S)-5-cyano-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrimidin-4-yl}benzenesulfonyl chloride (100 mg, 202 μmol) at room temperature, and the mixture was stirred for 3 h. The reaction mixture was then concentrated under reduced pressure and the residue was purified by preparative HPLC (column: Gromsil C-18; mobile phase: acetonitrile/water+0.1% TFA 10:90→90:10). This gave a colorless amorphous solid (56 mg, 58% of theory).

Provenance & Evidence