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Synthesis of aryl(di)azinyl ketones through copper- and iron-catalyzed oxidation of the methylene group of aryl(di)azinylmethanes.

Angewandte Chemie (International ed. in English) (2012-02-01)
Johan De Houwer, Kourosch Abbaspour Tehrani, Bert U W Maes
ABSTRAKT

Sustainable Oxidations: an oxidation method to transform aryl(di)azinylmethanes into aryl(di)azinyl ketones is described. Base metals (copper and iron) as catalysts in combination with O(2) as the oxidant are used, which makes this method sustainable. The utility of this method is illustrated by the synthesis of 6-(4-methylbenzoyl)pyridine-2-carbaldehyde, which is an intermediate in the preparation of the drug Acrivastine.

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Sigma-Aldrich
Acrivastine, ≥98% (HPLC)
Sigma-Aldrich
Triprolidine hydrochloride, ≥99%