反应详情

Compound 20 (0.88 g, 3.2 mmol) and 2-thiopheneboronic acid (0.87 g, 3.4 mmol) were dissolved in tetrahydrofuran (12 mL) and a 2 M-aqueous solution (4.2 mL) of sodium carbonate. To this solution, trans-bromo(N-succinimidyl)bis(triphenylphosphine)palladium(II) [trans-PdBr(N-Succ)(PPh3)2] (27.5 mg, 1.0 mol %) was added and treated in the same manner as in Example 11. The obtained residue was subjected to silica gel column chromatography and elution with an n-hexane/ethyl acetate (20:1) solution followed by conventional hydrolysis with potassium hydroxide to give 0.75 g (85%) of compound (22b) of interest as white solid.

1. additiontreated in the same manner as in Example 11
2. washThe obtained residue was subjected to silica gel column chromatography and elution with an n-hexane/ethyl acetate (20:1) solution
3. customfollowed by conventional hydrolysis with potassium hydroxide