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.
The conversion of N-benzylacrylamides to a diverse range of azaspirocycles is presented.
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.
We report an approach to build 2-spiropiperidine moieties starting from dihydropyridones through a tandem triflation–allylation reaction followed by ring-closing metathesis and then Pd-catalyzed functionalization.