Research On The Asymmetric Synthesis Of Cf₃-Containing Spiro-Oxindole-Pyrrolidine-Pyrazolone Compounds

Among various heterocyclic compounds,pyrazole derivatives are one of important nitrogen-containing heterocyclic compounds.In recent years,these compounds have been widely used in synthetic pharmaceuticals and agricultural products,and have been used as an important intermediate in organic synthesis.Chelating agents in bulk and coordination chemistry have received wide attention.Pyrazolonone is one of the pyrazole heterocyclic compounds with important biological activities,and has been studied for more than a century.As early as 1883,Ludwig Knorr first synthesized dimethylphenylpyrazolone(drug name: antipyrine)and determined it was the first antipyretic analgesic.In view of the continuing demand for new drugs,this special structural element containing a-CF3 group has also been introduced into a variety of drug backbones to enhance the biological activity of the drug or to improve the physicochemical properties of the compound,such as lipophilic or alkaline.It may also have a substantial impact on the conformation of the molecule.Moreover,some of the obtained new compounds containing a-CF3 group show promising biological activities.The pyrrolidine-spiroxane unit is a special heterocyclic structure which is the core structure of many natural families of alkaloids.Compounds with such structures tend to have a strong biological activity spectrum.Ongoing research has shown that such heterocyclic compounds have the potential to become drugs or bio-probes,which has generated a strong interest in the synthesis and development of related compounds.Pyrazolone,pyrrolidine,and-CF3 substituted oxindole units are the dominant structures in many biological compounds.The combination of the dominant structure into an organic molecule to discover a drug with medical value is one of the modern drug development studies.hot spot.For the above reasons,we use the trifluoromethyl-containing oxindole and pyrazolone structure for asymmetric [3+2] cycloaddition reaction.Under mild reaction conditions,quinine-derived amide is organic.The catalyst is highly stereoselective to perfectly combine the structures of oxindole,pyrazolone and pyrrolidine to construct a pyrrolidine structure,which is highly stereoselective to perfectly combine the structures of oxindole,pyrazolone and pyrrolidine.This class of compounds has four consecutive chiral carbon centers,two of which are continuous quaternary carbons.