Recent Advances in Catalytic Enantioselective Synthesis of Pyrazolones with a Tetrasubstituted Stereogenic Center at the 4-Position

Pyrazolone [2,4-dihydro-3H-pyrazol-4-one] represents one of the most important five-membered nitrogen heterocycles which is present in numerous pharmaceutical drugs and molecules with biological activity. Recently, many catalytic methodologies for the asymmetric synthesis of chiral pyrazolones have been established with great success, specially, for the synthesis of pyrazolones bearing a tetrasubstituted stereocenter at C-4. This review summarizes these excellent research studies since 2018, including representative examples and some mechanistic pathways explaining the observed stereochemistry.

Automated summary

Pyrazolone is an important nitrogen heterocycle found in pharmaceutical drugs and molecules with biological activity. Recent advancements have led to successful catalytic methodologies for asymmetric synthesis of chiral pyrazolones, particularly those with a tetrasubstituted stereocenter at C-4.