反应详情

Using the same procedure described in Example 1 but starting from 2-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol (Losartan)(2.13 g, 5.04 mmol) and 4-(nitrooxy)butanoic acid pentafluorophenyl ester (1.59 g, 5.04 mmol) TEA (0.7 ml, 5.04 mmol), DMAP (0.615 g, 5.04 mmol) and using DMF as solvent. Then the mixture was diluted with buffer solution (pH=3); the pH was adjusted to 2-3 and the mixture was extracted with EtOAc. The organic phase washed with brine, dried over Na2SO4 and evaporated. The residue was purified with Flash chromatography of the residue (CH2Cl2/MeOH 98:2) and the title compound was obtained as a white solid (1.48 g, 53%).

1. extractionthe mixture was extracted with EtOAc
2. washThe organic phase washed with brine
3. dry with materialdried over Na2SO4
4. customevaporated
5. customThe residue was purified with Flash chromatography of the residue (CH2Cl2/MeOH 98:2)