反应详情

Combine 5-Amino-1-(3,5-bis-trifluoromethyl-benzyl)-1H-imidazole-4-carboxylic acid amide (0.106 g, 0.30 mmol) and p-toluenesulfonyl chloride (0.069 g, 0.36 mmol) in pyridine (0.1 M), and stir at RT. After 2 h, quench the reaction with MeOH and concentrate. Redissolve in EtOAc, wash with H2O and brine, then dry (MgSO4), filter, and concentrate. Purify by radial chromatography on silica gel to give the title compound. MS (ES) 335.1 (M+1); 1H NMR (300 MHz, CD3OD): δ 7.96 (s, 1H), 7.77 (s, 2H), 7.37 (s, 1H), 5.31 (s, 2H).

1. customquench
2. customthe reaction with MeOH
3. concentrationconcentrate
4. dissolutionRedissolve in EtOAc
5. washwash with H2O and brine
6. dry with materialdry (MgSO4)
7. filtrationfilter
8. concentrationconcentrate
9. customPurify by radial chromatography on silica gel