Реакция #62409

Уравнение реакции

5-bromo-6-fluoro-3-iodo-1-trityl-1H-indazole

4-fluorostyrene

2-(di-ter-butylphosphino)biphenyl

triethylamine

→

title compound

Выход 74.1%

5-Bromo-6-fluoro-3-[(E)-2-(4-fluorophenyl)vinyl]-1-trityl-1H-indazole

Выход 74.1%

Растворители

ethyl acetate

N,N-dimethylformamide

Условия реакции

Обработка

1. 1
   Промывкаwashing successively with aqueous ammonium chloride and saturated brine
2. 2
   Сушкаdrying over anhydrous magnesium sulfate
3. 3
   Другоеthe solvent was evaporated
4. 4
   ДругоеThe residue was purified
5. 5
   Другоеseparated by silica gel column chromatography (ethyl acetate:n-hexane=1:100)

Методика

A solution of 3.0 g of 5-bromo-6-fluoro-3-iodo-1-trityl-1H-indazole, 628 mg of 4-fluorostyrene, 115 mg of palladium acetate, 307 mg of 2-(di-ter-butylphosphino)biphenyl and 3.60 mL of triethylamine in N,N-dimethylformamide was stirred at 70° C. for a day. After diluting with ethyl acetate, washing successively with aqueous ammonium chloride and saturated brine, and drying over anhydrous magnesium sulfate, the solvent was evaporated. The residue was purified and separated by silica gel column chromatography (ethyl acetate:n-hexane=1:100), to afford 2.2 g of the title compound as colorless crystals.

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