1403850-91-8Relevant articles and documents
Electrolytic macrocyclizations: Scalable synthesis of a diazonamide-based drug development candidate
Ding, Hui,Deroy, Patrick L.,Perreault, Christian,Larivée, Alexandre,Siddiqui, Arshad,Caldwell, Charles G.,Harran, Susan,Harran, Patrick G.
, p. 4818 - 4822 (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.