Chemical Properties
clear yellow or pink liquid
Uses
3-Fluoroiodobenzene was used to prepare methyl 4-iodobenzo[
b]thiophene-2-carboxylate, key intermediate for the synthesis of 4-substituted benzo[
b]thiophene-2-carboxamidines.
General Description
3-Fluoroiodobenzene participates in palladium-catalyzed hydroarylation of arylpropiolamides.
Synthesis
The general procedure for the synthesis of m-fluoroiodobenzene from 3-fluoroaniline was as follows: an aqueous solution (20 mL) of NaNO2 (6.4 g, 92.75 mmol) was slowly added dropwise at 0 °C to a solution of 3-fluoroaniline (10 g, 90.09 mmol) dissolved in 32% H2SO4 (179 g). The reaction mixture was stirred continuously at 0 °C for 1 hour. Subsequently, an aqueous solution (30 mL) of KI (22.4 g, 134.94 mmol) was added while maintaining 0 °C and stirring was continued at 0 °C for 1 hour. After completion of the reaction, the aqueous phase was extracted with EtOAc (2 x 250 mL). The organic phases were combined and washed sequentially with water (5×200mL) and 10% NaHSO3 solution (3×200mL), dried over Na2SO4 and concentrated under reduced pressure to remove the solvent, yielding 17.7 g of 1-fluoro-3-iodobenzene as a yellow solid in 82% yield.
References
[1] Patent: WO2008/103615, 2008, A1. Location in patent: Page/Page column 40
[2] Journal of the American Chemical Society, 1963, vol. 85, p. 709 - 724