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Open AccessIron-catalyzed stereoselective C–H alkylation for simultaneous construction of C–N axial and C-central chirality
The assembly of chiral molecules with multiple stereogenic elements is challenging, and, despite of indisputable advances, largely limited to toxic, cost-intensive and precious metal catalysts. In sharp contra...
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Open AccessLate-stage meta-C–H alkylation of pharmaceuticals to modulate biological properties and expedite molecular optimisation in a single step
Catalysed C–H activation has emerged as a transformative platform for molecular synthesis and provides new opportunities in drug discovery by late-stage functionalisation (LSF) of complex molecules. Notably, s...
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Article
Open AccessStereoselective assembly of C-oligosaccharides via modular difunctionalization of glycals
C-oligosaccharides are found in natural products and drug molecules. Despite the considerable progress made during the last decades, modular and stereoselective synthesis of C-oligosaccharides continues to be ...
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Article
Room temperature photo-promoted iron-catalysed arene C–H alkenylation without Grignard reagents
Iron is inexpensive, non-toxic and the most abundant transition metal in the Earth’s crust, rendering iron-catalysed C–H activations attractive yet particularly challenging. Despite major advances, iron-cataly...
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Open AccessLate-stage synthesis of heterobifunctional molecules for PROTAC applications via ruthenium-catalysed C‒H amidation
PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules emerging as a powerful modality in drug discovery, with the potential to address outstanding medical challenges. However, the synthetic...
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Article
Radical approach for enantioselective amination
Enantioselective electrocatalysis is emerging as an increasingly versatile tool in organic synthesis. Now, by applying asymmetric Lewis acid catalysis with an elaborated ligand design, radical electrochemical ...
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Open AccessElectrocatalyzed direct arene alkenylations without directing groups for selective late-stage drug diversification
Electrooxidation has emerged as an increasingly viable platform in molecular syntheses that can avoid stoichiometric chemical redox agents. Despite major progress in electrochemical C−H activations, these aren...
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Electrolyser design controls position-divergent C-H carboxylation
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Open AccessData-driven design of new chiral carboxylic acid for construction of indoles with C-central and C–N axial chirality via cobalt catalysis
Challenging enantio- and diastereoselective cobalt-catalyzed C–H alkylation has been realized by an innovative data-driven knowledge transfer strategy. Harnessing the statistics of a related transformation as ...
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Enantioselectivity prediction of pallada-electrocatalysed C–H activation using transition state knowledge in machine learning
Enantioselectivity prediction in asymmetric catalysis has been a long-standing challenge in synthetic chemistry because of the high-dimensional nature of the structure–enantioselectivity relationship. A lack o...
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Open AccessRecent advances in electrooxidative radical transformations of alkynes
During the past few years, electrochemical oxidative reactions through radical intermediates have emerged as an environmentally-benign, powerful platform for the facile formation of C–E (E = C, N, S, Se, O and...
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Article
Open AccessA recyclable stereoauxiliary aminocatalyzed strategy for one-pot synthesis of indolizine-2-carbaldehydes
Indolizine-carbaldehydes with the easily modifiable carbaldehyde group are important synthetic targets as versatile precursors for distinct indolizines. However, the efficient one-pot construction of trisubsti...
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Open AccessEfficient preparation of unsymmetrical disulfides by nickel-catalyzed reductive coupling strategy
Disulfides are widely found in natural products and find a wide range of applications in life sciences, materials chemistry and other fields. The preparation of disulfides mainly rely on oxidative couplings of...
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Open AccessC–H activation by immobilized heterogeneous photocatalysts
During the last decades, the merger of photocatalysis with transition metal chemistry has been surfaced as a sustainable tool in modern molecular syntheses. This Account highlights major advances in synergisti...
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Open AccessRhodaelectro-catalyzed access to chromones via formyl C–H activation towards peptide electro-labeling
Chromones represent a privileged scaffold in medicinal chemistry and are an omnipresent structural motif in natural products. Chemically encoded non-natural peptidomimetics feature improved stability towards e...
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Late-stage C–H functionalization offers new opportunities in drug discovery
Over the past decade, the landscape of molecular synthesis has gained major impetus by the introduction of late-stage functionalization (LSF) methodologies. C–H functionalization approaches, particularly, set ...
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C–H activation
Transition metal-catalysed C–H activation has emerged as an increasingly powerful platform for molecular syntheses, enabling applications to natural product syntheses, late-stage modification, pharmaceutical i...
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Open AccessChemodivergent manganese-catalyzed C–H activation: modular synthesis of fluorogenic probes
Bioorthogonal late-stage diversification of amino acids and peptides bears enormous potential for drug discovery and molecular imaging. Despite major accomplishments, these strategies largely rely on tradition...
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Nickela-electrocatalyzed sulfide and phosphine oxygenations with water
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Cobalt-catalysed C–H methylation for late-stage drug diversification
The magic methyl effect is well acknowledged in medicinal chemistry, but despite its significance, accessing such analogues via derivatization at a late stage remains a pivotal challenge. In an effort to mitig...
