Org. Lett. 2015, 17 (8), 1922-1925
DOI: 10.1021/acs.orglett.5b00608
Druzhenko T.; Denisenko O.; Kheylik Y.; Zozulya S.; Shishkina S. S.; Tolmachev A.; Mykhailiuk P. K.
A set of novel SO2-containing azabicyclo[3.n.1]alkanes has been synthesized by the double-Mannich annulation of of the corresponding monocyclic S-ketones. These compounds have been rationally designed as 3D-shaped, conformationally restricted SO2-containing building blocks for drug discovery.