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. 2011 Apr 27;133(16):6166-9.
doi: 10.1021/ja2014955. Epub 2011 Apr 5.

Selective activation of enantiotopic C(sp3)-hydrogen by means of chiral phosphoric acid: asymmetric synthesis of tetrahydroquinoline derivatives

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Selective activation of enantiotopic C(sp3)-hydrogen by means of chiral phosphoric acid: asymmetric synthesis of tetrahydroquinoline derivatives

Keiji Mori et al. J Am Chem Soc. .

Abstract

Chiral phosphoric acid-catalyzed asymmetric C-H functionalization has been achieved. In this process, enantiotopic C(sp(3))-hydrogen is selectively activated by chiral phosphoric acid to afford tetrahydroquinoline derivatives with excellent enantioselectivities (up to 97% ee).

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