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The early days of drug discovery and development were lonely: scientists in the 19th century made discoveries often driven by serendipity. Although fortuitous findings continue to happen, we currently rely on the synergistic collaboration across the organic and medicinal chemistry areas for accelerating the rational identification and design of lead compounds.
This collection showcases some of the most recent advances in the multidisciplinary field of discovery and development of bioactive compounds published in Nature Communications. The Medicinal Chemistry tab highlights additions to the med. chem. toolbox. Under Catalysis for Bioactive Compounds we acknowledge advances in homogeneous catalysis that open the door to obtaining bioactive compounds in higher quantity, quality and/or purity. Tying in with that, the Total Synthesis section contains reports on the complete chemical synthesis of natural products, still one of the best sources of drugs and drug leads. Last but not least, the Drug Biosynthesis section showcases some of the most recent discoveries of how Nature synthesizes bioactive compounds and how biocatalytic machinery can be exploited for chemical synthesis.
This collection will be regularly updated with studies published in Nature Communications that advance the field of medicinal and synthetic chemistry.
Axially chiral arylquinazolinones are structural motifs in several natural products and can also act as chiral ligands. Here, the authors show a chiral phosphoric acid-catalysed strategy to access enantiomerically pure arylquinazolinones by efficient transfer of central chirality into axial chirality.
Chiral pyridines are valuable building blocks in medicinal chemistry applications. Here, the authors report the copper-catalysed Lewis acid-assisted asymmetric alkylation of β-substituted alkenyl pyridines with Grignard reagents affording chiral pyridines with excellent enantioselectivity.
Electroreduction of CO2 to CO is a potential valorisation pathway of carbon dioxide for fine chemicals production. Here, the authors show a user-friendly device that couples CO2 electroreduction with carbonylation chemistry for up to gram scale synthesis of pharmaceuticals even under atmospheric CO2.
Methods for the asymmetric introduction of organofluorine groups are often limited by the lack of variability in the starting materials. Here the authors report an asymmetric radical process for the introduction of fluoroalkyl groups using readily available fluoroalkylated sulfonyl chlorides.
Biologically active compounds often contain a chiral centre in proximity of amine groups. Here, the authors developed a strategy involving asymmetric isomerization of allylic amines, enamine exchange and chemoselective reduction for the one-pot highly enantioselective synthesis of gamma-branched amines.
Transformations with ClCF2H are very limited and normally involve a difluorocarbene intermediate. Here, the authors report a nickel-catalyzed difluoromethylation of aryl chlorides with chlorodifluoromethane via a difluoromethyl radical intermediate and apply the method to the synthesis of marketed pharmaceuticals.
Selective para-functionalization of substituted arenes is a formidable challenge in homogeneous catalysis. Here, the authors achieved the para-selective C-H difluoromethylation of anilides, indolines and tetrahydroquinolines with a ruthenium catalyst in good yields and apply it to the synthesis of bioactive compounds.
Chemical transformation of amides is normally occurring under harsh conditions. Here, the authors report a mild iridium-catalyzed reductive Ugi-type coupling of tertiary amides, isocyanides and (thio)acetic acid or trimethylsilyl azide to give homologous, bioactive amine products.
Aryl sulfonamides and sultams are important pharmacophores in medicinal chemistry. Here, the authors report a practical palladium-catalyzed C–H activation assisted by amino-acid residues in the substrate leading to arylsulfonamides and bioactive peptidosulfonamide macrocycles.