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Montréal, Canada

Ding H.,University of California at Los Angeles | Deroy P.L.,Paraza Pharma Inc. 7171 | Perreault C.,Paraza Pharma Inc. 7171 | Larivee A.,Paraza Pharma Inc. 7171 | And 4 more authors.
Angewandte Chemie - International Edition | Year: 2015

An electrochemical method to synthesize the core macrolactam of diazonamides is described. Large ring-forming dehydrogenation is initiated by anodic oxidation at a graphite surface. The reaction requires no tailoring of the substrate and occurs at ambient temperature in aqueous DMF in an undivided cell open to air. This unique chemistry has enabled a concise, scalable preparation of DZ-2384; a refined analog of diazonamide A slated for clinical development as a cancer therapeutic. Electrifying chemistry! The core macrolactam of diazonamides can be synthesized electrochemically. This large ring forming dehydrogenation has enabled a concise preparation of DZ-2384, a refined analog of diazonamide A slated for clinical development as a cancer therapeutic. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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