C(N(CC)CC)C.[Cl:8][C:9]1[N:14]=[C:13](Cl)[C:12]([C:16]([F:19])([F:18])[F:17])=[CH:11][N:10]=1.Cl.[NH2:21][C@H:22]([CH3:26])[C@H:23]([OH:25])[CH3:24].[Na+].[Cl-]>C(#N)C>[Cl:8][C:9]1[N:14]=[C:13]([NH:21][C@H:22]([CH3:26])[C@H:23]([OH:25])[CH3:24])[C:12]([C:16]([F:19])([F:18])[F:17])=[CH:11][N:10]=1
4.8 ml (34.8 mmol) of triethylamine are added dropwise to 3.78 g (17.4 mmol) of 2,4-dichloro-5-trifluoromethylpyrimidine and 2.19 g (17.4 mmol) of (2R,3R)-3-amino-butan-2-ol hydrochloride in 70 ml of acetonitrile at 0° C. The mixture is slowly warmed to room temperature and then stirred for 48 hours. The mixture is added to half-concentrated NaCl solution and extracted with ethyl acetate. The combined organic phases are dried (Na2SO4), filtered and concentrated. The resulting residue is purified by HPLC. 1.45 g (5.4 mmol; 31% yield) of the product are obtained.
Loading…
