Reacción #595375

ord-9bb6984f92b749809f85999c622bd14c

Ecuación de reacción

Brc1n[nH]c2ccccc12
3-bromoindazole
CCN(CC)CC
triethyl amine
O=S(=O)(Cl)c1ccccc1C(F)(F)F
2-(trifluoromethyl)benzenesulfonyl chloride
O=S(=O)(c1ccccc1C(F)(F)F)n1nc(Br)c2ccccc21
3-bromo-1-(2-(trifluoromethyl)phenylsulfonyl)-1H-indazole
Rendimiento 86.9%

Disolventes

Condiciones de reacción

Condiciones detalladas
See reaction.notes.procedure_details.

Tratamiento posterior

  1. 1
    ConcentraciónThe reaction mixture was concentrated under reduced pressure
  2. 2
    Otrothe residue was purified on SiO2 using 5% to 20% ethyl acetate in heptane

Procedimiento

To a suspension of 3-bromoindazole (500 mg, 2.54 mmol) in 8 ml CH2Cl2 was added triethyl amine (1.06 ml, 7.61 mmol) at room temperature. To this yellow solution was added 2-(trifluoromethyl)benzenesulfonyl chloride (0.392 ml, 2.54 mmol) and the reaction mixture was stirred for 3 h at room temperature. The reaction mixture was concentrated under reduced pressure and the residue was purified on SiO2 using 5% to 20% ethyl acetate in heptane to give 3-bromo-1-(2-(trifluoromethyl)phenylsulfonyl)-1H-indazole (894 mg)

Fuente

DOI: 10.6084/m9.figshare.5104873.v1Patente: US09095583B2uspto-grants-2015_08