A parallel solution-phase synthesis of substituted 3,7-diazabicyclo[3.3.1]nonanes.
The parallel solution-phase synthesis of a series of building blocks and combinatorial libraries based on natural bispidine scaffold has been accomplished. Key reactions include catalytic hydrogenation of the (-)-cytisine heterocyclic system, followed by alkali-mediated ring cleavage. Using this approach, a series of new bispidine core building blocks for combinatorial synthesis with three points of diversity were effectively synthesized. The libraries from libraries were then obtained in good yields and purities using solution-phase acylation reactions. Obtained combinatorial libraries of 3,4,7-trisubstituted bispidines are potentially useful in the discovery of novel physiologically active compounds.
Ivachtchenko
Alexander V
AV
Chemical Diversity Labs Inc., 11558 Sorrento Valley Road, Suite 5, San Diego, California 92121, USA. av@chemdiv.com
Tkachenko
Sergey E
SE
Sandulenko
Yuriy B
YB
Vvedensky
Vladimir Y
VY
Khvat
Alexander V
AV