Oxidative ipso Substitution of 2,4-Difluoro-benzylphthalazines: Identification of a Rare Stable Quinone Methide and Subsequent GSH Conjugate from Novartis DMD 2012

Gunduz, M., et al.  Drug Metab. Dispos. 2012 Nov;40(11):2074-80

An interesting paper just came out from NIBR on DMD.

1. Two fluorine atoms was not able to block the P450-involved metabolism.

Instead, an oxidative ipso substitution occurs with the loss of a fluorine atom.

2. A resonance-stabilized quinone methide metabolite was identified.

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