反应详情

[(2-chlorophenyl)methyl]sulfonyl chloride (0.14 g, 0.6 mmol) was added to a mixture of ethyl 4-{2-[2-(2-Aminoethyl)-1-benzhydryl-5-chloro-1H-indol-3-yl]-ethoxy}-2-fluoro-benzoate (Step 6, Example 190, 0.12 g, 0.2 mmol) and K2CO3 (0.11 g, 0.8 mmol) in CH2Cl2 (2 mL) and water (1 mL) with stirring. After 2 hour at room temperature, the mixture was extracted with CH2Cl2 (10 mL) and the extract was washed with 0.5 N NaOH, and brine and dried over sodium sulfate. The CH2Cl2 solution was filtered through silica gel and the filtrate was evaporated. The resulting residue was triturated with a mixture of ether and hexanes to give 0.07 g of ethyl 4-{2-[1-benzhydryl-5-chloro-2-(2-{[(2-chlorobenzyl)sulfonyl]amino}ethyl)-1H-indol-3-yl]ethoxy}-2-fluorobenzoate as a white solid.

1. extractionthe mixture was extracted with CH2Cl2 (10 mL)
2. washthe extract was washed with 0.5 N NaOH, and brine
3. dry with materialdried over sodium sulfate
4. filtrationThe CH2Cl2 solution was filtered through silica gel
5. customthe filtrate was evaporated
6. customThe resulting residue was triturated with a mixture of ether and hexanes