Synthesis and characterisation of new antimalarial fluorinated triazolopyrazine compounds

• Kah Yean Lum,
• Jonathan M. White,
• Daniel J. G. Johnson,
• Vicky M. Avery and
• Rohan A. Davis

Beilstein J. Org. Chem. 2023, 19, 107–114, doi:10.3762/bjoc.19.11

• , Australia Discovery Biology, Griffith University, Nathan, QLD 4111, Australia NatureBank, Griffith University, Nathan, QLD 4111, Australia 10.3762/bjoc.19.11 Abstract Nine new fluorinated analogues were synthesised by late-stage functionalisation using Diversinate™ chemistry on the Open Source Malaria (OSM

• improve solubility and metabolic stability while retaining potency [5]. Late-stage functionalisation (LSF) is a strategy involving the use of C–H bonds as chemical handles for the introduction of various functional groups, which has been widely employed by medicinal chemists to generate new analogues of

Applications of organocatalysed visible-light photoredox reactions for medicinal chemistry

• Michael K. Bogdos,
• Emmanuel Pinard and
• John A. Murphy

Beilstein J. Org. Chem. 2018, 14, 2035–2064, doi:10.3762/bjoc.14.179

• mechanistic considerations are highlighted in the text when appropriate. Keywords: C–H functionalisation; heterocycles; late-stage functionalisation; medicinal chemistry; organic dyes; organic photocatalysts; peptide chemistry; photoredox catalysis; Review 1 Introduction 1.1 Main advantages of

• are better suited to be included in the late stage functionalisation (LSF) section. 2.4 Reactions manipulating hydrocarbon backbones The reactions of hydrocarbons are central to building the scaffolds of molecules. This is also true in medicinal chemistry. There are countless C–C bond-forming

• , milder conditions are employed and easily elaborated structures are accessed in one step. 4 Late stage functionalisation In this section, the bonds formed during the reactions are highlighted in red, as they are not always immediately and easily identifiable. Late stage functionalisation (LSF) is a