0000000000623649

AUTHOR

Myriam Ciordia

showing 3 related works from this author

ChemInform Abstract: A Versatile Approach to CF3-Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis o…

2016

The synthesis of new fluorinated pyrrolidones starting from unprotected amino esters and amino nitriles through a Michael addition-lactamization sequence is described. The resulting CF3 -containing building blocks, bearing a quaternary stereogenic center adjacent to the fluorinated group, have been converted into amino pyrrolidines that display potent β-secretase 1 (BACE1) inhibitory activity. This work constitutes an example of selective fluorination as a valid strategy for the modulation of physicochemical and biological properties of lead compounds in drug discovery.

Amidinechemistry.chemical_compoundTandemchemistryAmino estersDrug discoveryBiological propertyMichael reactionSequence (biology)General MedicineCombinatorial chemistryStereocenterChemInform
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Cover Picture: A Versatile Approach to CF3-Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis of Amid…

2015

AmidineExemplificationchemistry.chemical_compoundchemistryTandemStereochemistryOrganic ChemistryMichael reactionCover (algebra)General ChemistryCombinatorial chemistryCatalysisChemistry - A European Journal
researchProduct

A Versatile Approach to CF3-Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis of Amidine Class BACE1…

2015

The synthesis of new fluorinated pyrrolidones starting from unprotected amino esters and amino nitriles through a Michael addition-lactamization sequence is described. The resulting CF3 -containing building blocks, bearing a quaternary stereogenic center adjacent to the fluorinated group, have been converted into amino pyrrolidines that display potent β-secretase 1 (BACE1) inhibitory activity. This work constitutes an example of selective fluorination as a valid strategy for the modulation of physicochemical and biological properties of lead compounds in drug discovery.

Hydrocarbons FluorinatedMolecular StructureTandemAmino estersDrug discoveryStereochemistryOrganic ChemistryAmidinesStereoisomerismSequence (biology)General ChemistryCombinatorial chemistryPyrrolidinonesCatalysisStereocenterAmidinechemistry.chemical_compoundchemistryCyclizationBiological propertyDrug DiscoveryMichael reactionAspartic Acid EndopeptidasesAmyloid Precursor Protein SecretasesChemistry - A European Journal
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