反应详情

A solution of (3,5-dimethyl-4-{2-[3-methyl-4-(2,2,2-trifluoro-ethoxy)-pyridin-2-ylmethanesulfinyl]-benzimidazole-1-sulfonyl}phenoxy)acetic acid 2-(toluene-4-sulfonyl)ethyl ester (Intermediate 14, 400 mg, 0.50 mmol) and NaHCO3 (51 mg, 0.60 mmol, 1.2 eq) in THF-H2O (6 mL-3 mL) was heated to 70° C. for 3 h. Then volatile materials were removed, the residual gummy oil was dissolved in THF and the mixture was filtered to remove un-dissolved solid. The filtrate was dried, the solvent was removed by evaporation to give a yellow foam which was treated with ether-EtOAc (5:1) to precipitate a solid. The solid was treated with CH3CN, and then collected by filtration to give Compound 5 (230 mg, 72%) as a light yellow solid.

1. customThen volatile materials were removed
2. dissolutionthe residual gummy oil was dissolved in THF
3. filtrationthe mixture was filtered
4. customto remove
5. dissolutionun-dissolved solid
6. customThe filtrate was dried
7. customthe solvent was removed by evaporation
8. customto give a yellow foam which
9. customto precipitate a solid
10. additionThe solid was treated with CH3CN
11. filtrationcollected by filtration