反应详情

3-chloro-6-(4-methoxyphenyl)-9H-pyrido[2,3-b]indole (50 mg, 0.16 mmol, 1 equiv.), 3-nitrophenylboronic acid (81 mg, 0.48 mmol, 3 equiv.), K3PO4 (136 mg, 0.64 mmol, 4 equiv.), S-PHOS (13.1 mg, 0.032 mmol, 0.2 equiv.), Pd(OAc)2 (4.0 mg, 0.016 mmol, 0.1 equiv.) are introduced in a schlenk tube which is flushed with N2. Freshly distilled dioxane (0.433 ml) is then injected and the reaction is carried out at 100° C. overnight. The mixture is filtered through celite and concentrated under reduced pressure. The crude product is purified over silica gel chromatography (eluant CH2Cl2/AcOEt 6:4). The white solid obtained is washed with methanol to give the product as a white solid (43 mg, 0.11 mmol) in 69% yield.

1. customis flushed with N2
2. filtrationThe mixture is filtered through celite and
3. concentrationconcentrated under reduced pressure
4. customThe crude product is purified over silica gel chromatography (eluant CH2Cl2/AcOEt 6:4)
5. customThe white solid obtained
6. washis washed with methanol