A practical divergent synthetic approach is reported for the library of regio- and stereoisomers of glutamic acid analogs built on the spiro[3.3]heptane scaffold.
Serine/threonine kinase PLK4, a critical regulator of centrosome duplication, is closely associated with tumorigenesis due to its role in centrosome amplification.
A visible-light promoted cascade cyanoalkylsulfonylation/ipso-cyclization of N-arylpropiolamides toward sulfonated spiro[4,5]trienones via SO2 insertion was developed.
A cascade annulation of N-phenylpropiolamides with diselenides leading to the construction of 3-arylselenenyl spiro[4.5]trienones was realized under mild conditions with Selectfluor as the sole oxidant.
According to DFT calculations, the synthesis of spirocyclic σ1 ligands involves two aza-Michael additions or a [4 + 2] cycloaddition. Dispiro ligand with a high number of sp3 C-atoms shows promising σ1 affinity, selectivity and physicochemical properties.