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Published June 21, 2007 | Supplemental Material
Journal Article Open

A Facile and Modular Synthesis of Phosphinooxazoline Ligands


The copper(I) iodide catalyzed phosphine/aryl halide coupling procedure of Buchwald et al. provides modular, robust, and scaleable access to phosphinooxazoline (PHOX) ligands. The advantages of this method are highlighted by the convenient synthesis of PHOX ligands with varied steric and electronic properties, which would be challenging to synthesize by other protocols.

Additional Information

© 2007 American Chemical Society. Received 16 April 2007. Published online 31 May 2007. Published in print 1 June 2007. The authors gratefully acknowledge Ono Pharmaceutical Co., Ltd. (postdoctoral fellowship to K.T.), The Fannie and John Hertz Foundation (predoctoral fellowship to D.C.B.), Eli Lilly and Co. (predoctoral funding to R.M.M.), California Institute of Technology, and Abbott, Amgen, Bristol-Myers Squibb, and Merck for financial support.

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