Themed collection New Talent

Review covering the synthesis of 5- and 6-membered as well as condensed heteroarenes, focussing on the combinations in cooperative catalytic systems in strategies used to achieve selectivity and also highlights the mode of action for the cooperative catalysis leading to the synthesis of commercially and biologically relevant heteroarenes.

This review discusses the use of several ArSO₂SR_f reagents as SR_f sources, an emerging trend to access SR_f-containing molecules.

Peptide–oligonucleotide conjugates (POCs) are covalent constructs that link a molecule like DNA to a synthetic peptide sequences.

The role of silver salts in Pd-catalysed C–C bond forming transformations.

Intermolecular alkene difunctionalizations for the direct synthesis of saturated heterocycles.

Factors that affect the efficiency of amine transaminase catalyzed reactions using isopropylamine as an amine donor.

Rearranged ergostane-type natural products are structurally intriguing and exhibit biologically relevant properties.

Diversity-oriented synthesis adds biological performance as a new diversity element.

The review highlights the recent advances (2013-present) in the use of earth-abundant first row transition metals in homogeneous borrowing hydrogen catalysis.

The direct decarboxylative azidation of cyclic α-amino acids has been achieved via visible light-mediated organo-photoredox catalysis.

We report a high-affinity photoswitchable DNA binder, which displays different nucleosome-binding capacities upon visible-light irradiation.

Exposure of BIANFeCl₂ to nBuLi generates an anionic complex which is a competent catalyst for the selective reduction of esters to alcohols.

A new fluorogenic probe based on the recently identified 2,5-diaminopyrimidine (C4N4) fluorophore is introduced for azide-specific labelling.

Herein we report synthesis of complex heparan sulfate oligosaccharide precursors by automated glycan assembly using disaccharide donor building blocks.

Construction of structurally diverse carbazoles and bis-carbazoles by protecting-group-free formal [4 + 2]-benzannulation of 2-alkenyl indoles and aldehydes is demonstrated.

Tyrosine analogues containing an olefin moiety can be adenosylated by L-tyrosine lyases.

An alternative protocol for the B-alkyl Suzuki–Miyaura reaction to produce cyclic α,β-disubstituted enones is reported.

Herein we describe the direct enantioselective Lewis base/Pd catalysed α-allylation of pyrrole acetic acid esters.

Spin labeling of in vitro transcribed RNA by iEDDA click chemistry is demonstrated. This allows the determination of distance distributions between two nitroxide spin labels by PELDOR in a self-complementary RNA duplex.

Direct arylation and heteroarylation of unprotected tetrahydroisoquinolines were achieved under conditions free of metals, oxidants and solvents.

A fluorescent peptide displacement assay combined with statistical analysis is used for screening small molecules against different RNA targets and profiling their affinity/selectivity patterns.

A simple protocol for copper-catalyzed arene amination using aqueous ammonia without any additional ligands and organic coordinating solvents has been developed.

Quantum mechanical calculations (DLPNO-CCSD(T) and M06-2X) are employed to gain insights into the mechanism and selectivity in the catalytic synthesis of dihydropyrido[1,2-a]indoles from the cascade reaction between nitrones and allenes.

An efficient multicomponent dipolar cycloaddition for the synthesis of polycyclic fused pyrrolizidines was developed using N-aromatic zwitterions, aldehydes, and amino acids.

Fluoroalkylated alkynes, which are versatile building blocks for the synthesis of various biologically active organofluorine compounds, were synthesized from easily available alkynyl halides and fluoroalkyl halides by visible-light photocatalysis.

We report the total synthesis of (±)-antroquinonol based on a concise and efficient route.

Chiral selenide-catalyzed enantioselective trifluoromethylthiolation of 1,1-disubstituted alkenes is disclosed. Various chiral trifluoromethylthiolated 2,5-disubstituted oxazolines were obtained in good yields with high enantioselectivities.

A simple and efficient iron-catalyzed protodehalogenation of alkyl and aryl halides using phenylhydrosilane is disclosed.

Simple cationic bis(phosphine)iridium complexes are shown to be highly selective catalysts for ether cleavage with silanes. Benzylic ethers can be cleaved under mild conditions in the presence of reductively-labile functional groups.

A one-pot oxidative cross-dehydrogenative [2 + 3] annulation of α-amino ketones with α-keto esters at room temperature is reported.

TfOH-catalyzed glycosylation with D-galactosaminyl N-phenyl trifluoroacetimidate as the donor was developed for the construction of the challenging β-(1 → 5)-linked GalNAc-Kdo disaccharide antigen from Kingella kingae KK01.

We present the functional characterization of GlbB, a lysine 4-hydroxylase from the glidobactin biosynthetic gene cluster.

A palladium-catalyzed intramolecular carboborylation of 1,3-diene has been developed for the synthesis of iminoindolines with a quaternary carbon centre.

Two new palladium-catalyzed reactions enabled the synthesis of the core structure of phalarine.

An operationally simple mechanochemical method for the Pd catalysed Buchwald–Hartwig amination of arylhalides with secondary amines has been developed using a Pd PEPPSI catalyst system.

An organocatalytic asymmetric cascade Michael/hemiketalization/acyl transfer reaction between (E)-2-(2-nitrovinyl)phenols and 1,3-propanediones is disclosed to generate products having keto, ester and nitro functionalities.

The first regioselective MBH-type α-alkylation of α,β,γ,δ-unsaturated aldehydes is achieved using diarylcarbinols with an excellent E/Z selectivity under mild reaction conditions.

We describe a palladium catalyzed salt-free decarboxylative aryl allylation of free benzoic acids with allyl tert-butyl-carbonates.

A universal “helping hand” to facilitate the synthesis of A chain of insulin-related peptides.

Synthetic studies into the origins of the alkaloid incargranine A have resulted in the development of a four-step (longest linear sequence) total synthesis.

Transition structure for the bifunctional thiourea catalyzed Michael addition using ¹³C KIEs and DFT calculations.

¹⁹F NMR-guided development of a BPTF chemical probe through SAR and ligand deconstruction.

Atom-economical and regioselective C(sp³)–C(sp³) bond formation has been achieved by C(sp³)–H alkylation of N,N-dimethyl anilines with sterically demanding alkenes by scandium catalysis.

Stable monoclonal antibodies are generated by the mild and efficient re-bridging of interchain disulfides using an isobutylene motif. Effector functions and pharmacokinetics of the stapled antibodies are maintained at a similar level as their native forms.

A minimalist fluorogenic probe is presented capable of the mapping of aldehydic load through live cell microscopy.

We report here that addition of stoichiometric amounts of alcohols or water to mixtures of imines and pinacolborane promote reduction reactions.

Spectroscopic and calorimetric study of DNA-binding by doxorubicin and doxorubicinone found different binding modes for the two molecules, despite their structural homology.

The oxime connection between linear peptides and hydrophobic aldehydes affords amphiphiles that are excellent biocompatible scaffolds for the hierarchical self-assembly of nano and micro fibrillar structures in aqueous media.

We report on the synthesis of a hemithioindigo molecular motor bearing thioether feet for metal surface attachment and a comprehensive study of its light induced unidirectional motion in solution.

Thioformamides are easily prepared – under full chemocontrol – through the partial reduction of isothiocyanates with the in situ generated Schwartz reagent.

The first total synthesis of myxocoumarin B along with its initial biological evaluation in antifungal and cytotoxicity assays are reported.

T3 and T4 DNA ligase have contrasting performance in ligase-catalysed oligonucleotide polymerisations.

We report a metal-free photocatalytic approach to the synthesis of glycoconjugates, highlighting the mild nature of the reaction conditions.

Reversibly photoswitchable discotic liquid crystals (DLCs) with no change in columnar assembly.

A controlled-release fertiliser was prepared by the inverse vulcanisation of canola oil in the presence of nitrogen, phosphorous and potassium nutrients.

The rhodium-catalyzed arylative cyclization of enone tethered-cyclohexadienones has been developed with high efficiency, thus providing cis-fused bicyclic enones in good yields and with excellent diastereoselectivities.

DFT calculations reveal the origins of axial chirality control by cinchona alkaloid derivatives.

A one-pot, regiospecific synthesis of dihydrofurans bearing a quaternary centre is developed from the formal [3 + 2] annulation of tert-propargyl alcohols and 1,3-diketones through the S_N2^I mechanism to form homoallenyl ketone and a subsequent cycloisomerization reaction.

Structural modulation of the fluorescent protein (FP) chromophore to enable fluorogenic probe for SNAP-tag towards wash-free live cell imaging.

A boronic acid-catalysed C-3 selective ring opening of 3,4-epoxy alcohols with thiophenols and thiols as nucleophiles has been accomplished.

Human milk oligosaccharides (HMOs) possess antimicrobial activity against a number of bacterial pathogens.

Efficient syntheses of 4-epi-galiellalactone and the corresponding activity-based probe enabled chemoproteomic studies to reveal the biological targets.

Computations reveal that the potential for aromaticity gain and loss in nucleobases play key roles in modulating base pairing strengths.

A strategy to diversely functionalize the C7-position of DMXAA has been developed as a means to discover potential human-STING agonists.

Peroxynitrite (ONOO⁻) is involved in a variety of physiological and pathological processes.

Diverse peptide sequences and folds promote cysteine arylation.

A mild and operationally simple methodology is reported for the synthesis of cyclobutane rings imbedded within a C2-symmetric tricyclic framework.