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A novel Cu( ii )-catalyzed and acid-promoted highly regioselective oxidation of tautomerizable C(sp 3 )–H bonds adjacent to 1-Bn-DHIQs was developed. This method was successfully applied in the first total synthesis of canelillinoxine.

rsc advances

Copper(<scp>ii</scp>)-catalyzed and acid-promoted highly regioselective oxidation of tautomerizable C(sp<sup>3</sup>)–H bonds adjacent to 3,4-dihydroisoquinolines using air (O<sub>2</sub>) as a clean oxidant

Copper(ii)-catalyzed and acid-promoted highly regioselective oxidation of tautomerizable C(sp3)–H bonds adjacent to 3,4-dihydroisoquinolines using air (O2) as a clean oxidant

Copper(ii)-catalyzed and acid-promoted highly regioselective oxidation of tautomerizable C(sp³)–H bonds adjacent to 3,4-dihydroisoquinolines using air (O₂) as a clean oxidant