反应详情

A solution of crude (4-{tert-butoxycarbonyl-[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-2-methyl-phenoxy)-acetic acid methyl ester (2.1 g containing 1.83 g, 3.32 mmol) in CH2Cl2 (33 ml) was treated at 0° C. with TFA (12.7 ml) and stirred at RT for 45 min. The reaction was evaporated, treated with chilled aqueous saturated NaHCO3 solution/Et2O (3×). The organic phases were washed with aqueous 10% NaCl, dried (Na2SO4) and evaporated. Purification by flash chromatography with a gradient of n-heptane:EtOAc 95:5 to 4:1 yielded 0.34 g of (2-methyl-4-{[4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethyl]-amino}-phenoxy)-acetic acid methyl ester as an light yellow solid, MS: 451.3 (MH+).

1. customThe reaction was evaporated
2. additiontreated with chilled aqueous saturated NaHCO3 solution/Et2O (3×)
3. washThe organic phases were washed with aqueous 10% NaCl
4. dry with materialdried (Na2SO4)
5. customevaporated
6. customPurification by flash chromatography with a gradient of n-heptane:EtOAc 95:5 to 4:1