反应详情

A suspension of (3aR,6aR)-tert-butyl hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate (85 mg, 0.40 mmol, prepared as described in WO2001081347), the product from Example 53A (97 mg, 0.37 mmol), tris(dibenzylideneacetone)dipalladium(0) (13.4 mg, 0.015 mmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (25 mg, 0.044 mmol) and cesium carbonate (190 mg, 0.58 mmol) in anhydrous dioxane (4 mL) was heated at 90° C. for 18 hours. The reaction mixture was cooled and filtered through a glass frit. The filtrate was concentrated and the residue was purified by silica gel chromatography (EtOAc, Rf=0.4) to afford the title compound. MS (APCI) m/z=445 (M+H)+.

1. temperatureThe reaction mixture was cooled
2. filtrationfiltered through a glass frit
3. concentrationThe filtrate was concentrated
4. customthe residue was purified by silica gel chromatography (EtOAc, Rf=0.4)