Browse Articles

Boronic esters are versatile intermediates that readily accept nucleophiles and then undergo 1,2-migration, expelling a neighbouring leaving group. Such reactivity enables carbon chains to be grown one atom at a time with high stereocontrol. This Review examines the fundamentals of lithiation–borylation methodology and its application to natural product synthesis.

During the liquid-to-solid transition of alloys with very small concentrations of a minor component, surface patterns emerge that feature enrichment of the minor component. These periodic surface patterns may be beneficial for the use of precious metals in surface science applications.

The α-arylation of ketones is a powerful synthetic strategy for the construction of C–C bonds, but general metal-free methods are scarce. Now, a green-light-mediated photoredox protocol enables this transformation, giving access to a broad range of useful building blocks and value-added biorelevant products.

The solidification of liquid metal alloys drives phase separation and pattern formation. Now, it emerges that the solidification of liquid metal alloys on a surface follows unique solidification patterns that reveal alternating convergent and divergent growth habits, leading to oscillatory bifurcation patterns.

Mild and metal-free direct α-arylation of ketones has long been a challenging transformation. Now, a metal-free photoredox approach has been developed using electron-rich acridinium ions to photoactivate C(sp²)–X bonds under low-energy green light and to catalyse the α-arylation of cyclic ketones. This approach is a multigram and sustainable methodology for the synthesis of pharmaceutical synthons.

Taking inspiration from palladium–norbornene cooperative catalysis, Catellani-type reactions are now performed using a hybrid olefin ligand with a P or S coordination site. This olefin ligand enables efficient ipso,ortho-difunctionalization of iodoarenes. Mechanistic studies show the formation of organopalladium intermediates that comprise both the substrate and the hybrid olefin ligand.

Sulfoximines and sulfonimidoyl groups have recently emerged as powerful pharmacophores, however, their synthesis and incorporation into complex molecules is typically limited by long synthetic routes and the need to control stereogenic S-centres. Now, a stereospecific S_NAr approach has been developed for the synthesis of α-(hetero)arylation of sulfonimidoyl motifs.

Asymmetric cyanation reactions promoted by chiral copper catalysts via a radical relay process are discussed in this Perspective. In particular, we outline the mechanisms of carbon radical formation and subsequent asymmetric radical cyanation reactions.

Environmentally beneficial reverse supply chains for chemicals, materials and devices are enablers of a sustainable future, writes Elsa Olivetti.

Welcome to the first issue of Nature Synthesis; a home for new and important syntheses of molecules and materials that can make the world a better place.

Predictably activating C–H and C–C bonds for the synthesis of new materials remains a challenge within the synthetic community. A ternary catalytic dance between radicals, metals and light may unlock this puzzle.

Late-stage tritiation with high selectivity, isotopic purity and functional-group tolerance is important for the radiolabelling of drug candidates or bioactive compounds. Now, a broadly applicable protocol using aryl thianthrenium salts allows for tritiation of complex molecules by hydrogenolysis via an intermediate cationic palladium complex.

Iterative synthesis can generalize, automate and democratize the molecule-making process. Now, by using a computer algorithm to scan the depths of chemical reactivity space, thousands of iterative ways to make small molecules are discovered.

The organizing principles of click chemistry help scientists make molecules for a variety of applications. Such democratization of synthesis is challenging and rewarding, as useful simplicity is difficult to achieve. We reflect on this and look forward, hoping to continue to tie the joy of functional discovery to the challenges of synthetic chemistry.

In early 2020, scientists and medics started rummaging around the pharmacy shelves hunting for treatments that might curtail the spiralling pandemic death rates. This is the story of how they are searching and what they have found so far.

Enzymes catalyse reactions with unparalleled activity and selectivity. Using chemical insights, researchers can now direct these powerful natural catalysts to perform new-to-nature transformations that solve challenging synthetic problems. In this Perspective, we show how chemists and protein engineers have guided nature’s genetically encoded and evolvable machinery to perform new biocatalytic transformations.

Iterative sequences of organic reactions can be automated but are rare and challenging to identify. Now, a computer-driven strategy is reported for the systematic discovery and evaluation of such sequences. Several of the iterative sequences are validated experimentally and enable the syntheses of useful motifs in natural product targets.