Chemistry Research Updates: Late-Stage Functionalisation, Molecular Glue & Ketone Homologation
Research highlights from week 36/2026
Molecular Editing Reveals a Bilobalide Chemotype that Attenuates Prolyl Endopeptidase (PREP)-Linked Neuroinflammation
Natural products offer privileged three-dimensional chemotypes for drug discovery, yet scaffold lability and limited analogue space often impede mechanism-guided optimization. …
chanin-sillapachaiyaporn
Total Synthesis of Complex Natural Products
Total synthesis stands as one of the most intellectually demanding and logistically challenging disciplines within organic chemistry. Unlike highly applied branches such as process …
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4 min read
Molecular editing of bilobalide: Regioselective C-ring lactam formation
Late-stage diversification of complex natural products enables rapid access to analogues for structure-activity relationship studies. Herein, we report a regioselective …
wenjing-wang
Antiviral profiling and cellular activation of carbobicyclic nucleoside analogues
Nucleoside analogues are important antiviral and anticancer agents. In this study, we investigated a new class of nucleoside analogues built on a synthetically accessible …
Deracemisation lead to enriched alpha Amino Aldehydes
Luo and coworkes from Tsinghua University report a novel method for deracemisation in JACS
Practical access to trisubstituted Morita‐Baylis‐Hillman‐type products through copper‐catalyzed reductive aldol reactions of alkynones
AbstractWe report a convenient and diastereoselective copper‐catalyzed reductive alkynone aldol addition to aldehydes, with pinacolborane as stoichiometric reductant, that results …
Lactone-to-lactam editing alters the pharmacology of bilobalide
Precise transformations of natural products (NPs) can fine-tune their physicochemical properties while preserving inherently complex and evolutionarily optimized parent scaffolds. …
xiaoding-jiang
Diastereo- and enantioselective construction of stereochemical arrays exploiting non-classical hydrogen bonding in enolborates
We report a copper-catalyzed reductive aldol addition to aldehydes and ketones, with pinacolborane as stoichiometric reductant, that results in the generation of stereodefined …
matthew-li
![Breaking the aromaticity of thiophene using a [4+3] cycloaddition featured image](/post/thiophene-angew-2024/featured_hu_950411bbaf1d50d7.webp)
Breaking the aromaticity of thiophene using a [4+3] cycloaddition
A novel dearomative, intramolecular [4+3]-cycloaddition of thiophenes at low temperatures yielding complex tricyclic ring systems.
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1 min read