113451-54-0Relevant articles and documents
A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane
Beinat, Corinne,Banister, Samuel D.,McErlean, Christopher S.P.,Kassiou, Michael
, p. 5345 - 5347 (2013)
The rigid piperazine homologue 2,5-diazabicyclo[2.2.1]heptane (DBH) finds extensive application in medicinal chemistry and pharmaceutical research, but access to this scaffold is non-trivial. This letter details a concise synthetic sequence that gives ready access to DBH on gram scale. The route features a Staudinger reduction of an azide to facilitate a transannular cyclisation.