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Nucleophilic aromatic substitution; 1,2-Bis(diphenylphosphino)benzene

SyntheticPage 556
DOI: 10.1039/SP556
Submitted May 02, 2012, published May 07, 2012
Alex Henderson (Alex.Henderson@bris.ac.uk)
A contribution from Bristol Chemical Synthesis DTC


			Reaction Scheme: Nucleophilic aromatic substitution

Chemicals Used

Potassium diphenylphosphide solution, 0.5 M in THF (Sigma-Aldrich)
1,2-Difluorobenzene, 98% (Sigma-Aldrich) 
PhMe (Grubbs Solvent System - passed through passed column of alumina)
Activated charcoal (Sigma-Aldrich)

Procedure

To an anhydrous 0.5 M THF solution of potassium diphenylphosphide (45.0 mL, 22.5 mmol) at RT, was added 1,2-difluorobenzene (1.97 mL, 20.0 mmol) and anhydrous N2 saturated PhMe (50.0 mL). The resulting solution was heated to reflux (110 °C) for 5 h, by which time the dark red colour of the phosphide had dissipated, and 19F NMR spectroscopy showed a single environment (δF: -103.3, d, JFP = 53.0 Hz) correlating to a monophosphine species.§ To the solution at RT, was added an anhydrous 0.5 M THF solution of potassium diphenylphosphide (45.0 mL, 22.5 mmol) and left to reflux (110 °C) for 15 h. P NMR spectroscopy revealed a single peak (δp: -12.3) and the red/orange reaction mixture was concentrated in vacuo. The residue was suspended in PhMe (200 mL) at 70 °C, and activated charcoal (≈ 5.0 g) was added, whilst vigorous stirring occurred. The mixture was hot vacuum filtered through Celite and the solvent was removed in vacuo. The crude material was recrystallised (PhMe) to afford 1,2-bis(diphenylphosphino)benzene  (87%, 7.80 g) as a colourless solid.
 §No peak observed for 1,2-difluorobenzene  F: -138.7). P NMR spectrum showed concurrent data (δP: -18.0, d, JPF = 53.0 Hz).

Author's Comments

  • Glassware was oven dried (150 oC) prior to use.
  • Reaction performed under an atmosphere of N2 in purged apparatus.
  • NMR spectroscopy was carried out with aliquots from the reaction vessel (taken in an inert fashion) and later recombined. 
  • All chemicals were used without further purification however were checked for purity by 1H and 31P NMR spectroscopy.
  • KP(Ph)2  was transferred to a Young's flask, from the Sigma-Aldrich bottle, prior to use.
  • Celite filter additionally washed with hot (70 oC) PhMe (2 x 40 mL) as product precipitates in cool PhMe.
  • After recrystallisation, the solution was naturally left to cool to RT which caused precipitation of some material. The RBF was then refridgerated for 4 h which enhanced precipitation. Compound isolated by Buchner filtration.
  • Product is air stable.
 

Data

 νmax / cm-1 (film): 3056 (w), 1583 (w), 1567 (w), 1476 (m), 1435 (m), 1309 (w), 1157 (w), 1069 (w); mp 186-187 °C (PhMe) [Lit. 183-185 °C (PhMe / EtOH)]; δ(400 MHz, CDCl3): 6.97-7.02 (4H, m, ArCH), 7.08-7.22 (20H, m, ArCH); δC(100 MHz, CDCl3): 128.3 (t, J = 3.5 Hz, ArCH), 128.4 (ArCH), 129.1 (ArCH), 133.9 (t, J = 10.0 Hz, ArCH), 134.1 (t, J = 3.0 Hz, ArCH), 137.1 (t, J = 3.0 Hz, ArC), 143.7 (dd, J = 10.0 and 10.0 Hz, ArC); δ(121 MHz, CDCl3): -13.4.

Lead Reference

Baker, B. A.; Bošković, Ž. V.; Lipshutz, B. H. Org. Lett. 2008, 10, 289-292.

Other References

McFarlane, H. C. E.; McFarlane, W. Polyhedron. 1983, 2, 303-304.
Tunney, S. E.; Stille, J. K. J. Org. Chem. 1987, 52, 748-753.
 

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Keywords: aromatic nucleophilic substitution, aromatics/arenes, carbocyclic compounds, ligand, organo phosphorous

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