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Marco Bandini, Astrid Eichholzer, Michele Tragni and Achille Umani-Ronchi Enantioselective Phase-Transfer-Catalyzed Intramolecular Aza-Michael Reaction: Effective Route to Pyrazino-Indole Compounds Angewandte Chemie International Edition 47

Article first published online: 17 MAR 2008 | DOI: 10.1002/anie.200705685

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Producing polycycles: A mild and direct stereocontrolled route to pharmacologically active pyrazino-indol-1-ones has been developed. The optimal phase-transfer conditions provide variously functionalized ring-closed compounds in high chemical and optical yields (see scheme; X=H, F, Cl, Me, OMe; Ar=Ph, β-naphthyl; R′=tBu, Et, Me; R=benzyl, para-methoxyphenyl).

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