反应详情

To a solution of (S)-6-benzyloxymethyl-3-(4-fluoro-phenyl)-2-(6-methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole (0.3 g, 0.73 mmol) in chloroform (1.0 mL) is added trimethylsilyl iodide (0.173 mL, 1.21 mmol). The mixture is stirred 2 h, diluted with methanol (10 mL), stirred 10 min, and concentrated in vacuo. The residue is taken up in ethyl acetate (50 mL), washed with aqueous sodium thiosulfate (2×50 mL), saturated sodium bicarbonate solution, and brine. The resulting solution is dried (magnesium sulfate), filtered, and concentrated in vacuo. The residue is chromatographed on SiO2 (3% methanol/ethyl acetate) to yield the title compound, 149 mg (64%), as a pale yellow solid.

1. stirringstirred 10 min
2. concentrationconcentrated in vacuo
3. washwashed with aqueous sodium thiosulfate (2×50 mL), saturated sodium bicarbonate solution, and brine
4. dry with materialThe resulting solution is dried (magnesium sulfate)
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. customThe residue is chromatographed on SiO2 (3% methanol/ethyl acetate)