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The expansion of catalytic methods is a focus of contemporary interest due to the adverse effects of the manufacturing process of fine chemicals, pharmaceuticals, and materials on the environment. In...

The Structure Ligation Relationship (SLR) of free amino acids (AAs) under Pd‐catalysis were examined for the chemo‐ and regio‐selective indole C−H arylation reactions. While the majority of AAs were minor or ineffective, the L‐aspartic acid (L‐Asp) stands out promising to deliver high‐value C3‐arylated indoles with excellent chemo‐ (C vs N) and regioselectivity (C3 vs C2) with high functional group tolerance. Thus, the protocol offers a cost‐effective and sustainable alternative of phosphine‐based ligands for the indole C3−H arylation reactions. Preliminary mechanistic investigations suggested the simultaneous involvement of −NH2, α‐CO2H, and β‐CO2H functionalities of L‐Asp and found critical for its ligation efficiency. The developed catalytic system was compatible with the tandem decarboxylation/arylation procedure for the chemoselective synthesis of 3‐aryl indoles.magnified image

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With no proven therapy against COVID-19, the repurposing of existing drugs is an ongoing exercise. In this context, an antimalarial drug, hydroxychloroquine (HCQ) received immediate stardom when the US-FDA issued an Emergency Use Authorization (EUA) for HCQ against COVID-19 based on the limited clinical study. However, on 17 June 2020, WHO announced the stoppage of the HCQ trial for COVID-19 treatment based on data received from the Solidarity trial and UK's Recovery trials indicating HCQ does not result in the reduction of mortality of hospitalized COVID-19 patients when compared with standard of care. In this context, the present review aims to provide a developmental journey of HCQ including medicinal chemistry highlighting the essential pharmacology and the current studies exploring its effectiveness against COVID-19, and its synthetic advancement.