Methylamine → HCID 46928996, compound

Participants

Reaction Steps

Under an atmosphere of argon protective gas, 5-cyano-2-{(4S)-5-cyano-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrimidin-4-yl}benzenesulfonyl chloride (30 mg, 61 μmol) was dissolved in absolute THF (2 ml), a 2 M solution of methylamine in THF (91 μl, 182 μmol; 3 eq.) and triethylamine (6.1 mg, 61 μmol; 1 eq.) were added 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 (25 mg, 83% of theory).

Provenance & Evidence