Design of multivalent pharmacological chaperones against Pompe disease via metal-free ligation We report herein the design of multivalent pharmacological chaperones (PCs), based on d- and l-deoxynojirimycin (DNJ), to treat Pompe disease (PD), a lysosomal storage disorder caused by mutations in…

🔓Be sure to read this #OpenAccess paper from Cécile Dehoux et al. @cnrs.fr designing multivalent pharmacological chaperones against Pompe disease via metal-free ligation #orgchem #medchem

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A pre-synthetic conjugation methodology of DNA and RNA: combining on-column conjugation and tandem oligonucleotide synthesis Amino modifiers are valuable chemical tools for nucleic acid bioconjugation applications and for probing potential mechanisms relevant to the origins of life. Herein, we describe a streamlined and…

🔓Don't miss in our latest issue a #OpenAccess paper by Jagandeep S. Saraya & Derek K. O'Flaherty @uofguelph.bsky.social combining on-column conjugation and tandem oligonucleotide synthesis to enable a versatile conjugation TOS methodology #orgchem

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Tungsten-catalyzed continuous-flow oxidation of sulfides to sulfones with hydrogen peroxide Continuous-flow oxidation of sulfides to sulfones was achieved with hydrogen peroxide (H2O2) using a catalyst column, which was simply packed with a mixture of oxodiperoxotungstate-2,2′-bipyridine…

🔓Check out #OpenAccess research from Ken-ichi Fujita et al. at AIST in our latest issue achieving tungsten-catalyzed continuous-flow oxidation of sulfides to sulfones with hydrogen peroxide #orgchem

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Regioselective iridium(III)-catalyzed C–H cyclization using an acetylene surrogate: direct access to hydroxylated polycyclic phthalazinones An iridium(iii)-catalyzed C–H cyclization between N-arylphthalazinones and 2-chloroacetaldehyde has been developed. This reaction provides efficient access to tetracyclic phthalazine derivatives with…

Take a look at in our latest issue at a paper by Lin Dong & co. on regioselective iridium(iii)-catalyzed C–H cyclization using an acetylene surrogate for direct access to hydroxylated polycyclic phthalazinones #orgchem

📍Sichaun University

Peptide-directed solid-phase reductive amination We report an integrated solid-phase reductive amination/solid-phase fragment condensation (SPFC) strategy for the replacement of amide bonds in peptide sequences with the aminomethylene Ψ[CH2–NH]…

🔓Be sure to read this #OpenAccess paper in our latest issue from Spyridon Mourtas et al. at the University of Patras reporting peptide-directed solid-phase reductive amination #orgchem

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Transaminase-triggered synthesis of 2,5-disubstituted pyrrolidines 2,5-Disubstituted pyrrolidines were synthesised from ketoenone substrates using a transaminase-triggered intramolecular aza-Michael reaction in moderate to good yields. The pyrrolidines were isolated…

🔓Don't miss this #OpenAccess research by Marianne Bore Haarr, Elaine O'Reilly & co. @ucddublin.bsky.social in our latest issue describing the transaminase-triggered synthesis of 2,5-disubstituted pyrrolidines #orgchem

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📢Our latest issue is now online!

Check out the review behind the cover by Guru Prasad Rameshbabu & Sabbasani Rajasekhara Reddy at Vellore Institute of Technology looking at recent use of 4-chloro-2H-chromene-3-carbaldehyde as a scaffold in organic synthesis #orgchem

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Mn(III)-mediated oxidative cyclisation via C(sp3)–H functionalisation: an efficient strategy for benzo-fused aza-heterocycle synthesis We present an effective Mn(iii)-mediated approach for the C(sp3)–H functionalisation of N-aryl cyclic amines and their intramolecular coupling with a malonate partner. This methodology facilitates…

Be sure to read research from Dae Young Kim & co. at Soonchunhyang University in our latest issue using Mn(iii)-mediated oxidative cyclisation via C(sp3)–H functionalisationas an efficient strategy for benzo-fused aza-heterocycle synthesis #orgchem

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Biocatalytic synthesis of heterobiaryl sulfoxides: a comparative study between Baeyer–Villiger monooxygenases and unspecific peroxygenases The biocatalytic sulfoxidation of heterobiaryl indole- and pyrrole-based sulfides was investigated using unspecific peroxygenases (UPOs) and Baeyer–Villiger monooxygenases (BVMOs) as complementary…

🔓Don't miss in our latest issue a #OpenAccess paper by Alejandro González-Benjumea, Abel Ros, Gonzalo de Gonzalo et al. @unisevilla.us.es & @csic.es reporting the biocatalytic synthesis of heterobiaryl sulfoxides #orgchem

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Functionalized porphyrin–fullerene dyads: a pathway to the enhanced performance of perovskite solar cells Dyads consisting of a porphyrin with a bulky tert-butyl benzoate group linked to a fullerene cage through a biphenyl spacer were synthesized by the Prato reaction to fine-tune optoelectronic…

Check out a paper by Zheng-Chun Yin, Guan-Wu Wang & co. from the University of Science & Technology of China in our latest issue describing the synthesis of functionalized porphyrin–fullerene dyads #orgchem

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Green and sustainable nanocatalyzed syntheses of hybrid heterocyclic scaffolds with privileged substructures This review article presents recent advances relating to the use of nanostructured catalysts in the construction of drug-like small hybrid molecules with structural diversity and molecular complexity…

Take a look at this review in our latest issue from Mahendra Kumar et al. looking at the recent advances in nanocatalysed synthesis of hybrid heterocyclic scaffolds with privileged substructures #orgchem #medchem

📍University of Rajasthan

Selective functionalization of the 1,6-anhydro moiety and of the double bond of levoglucosenone Through a very efficient, step-economical (only 4 steps) and diastereoselective–chemoselective procedure, bio-based levoglucosenone has been converted into a versatile azide, which may be regarded as…

🔓Be sure to read in our latest issue this #OpenAccess paper from Luca Banfi & co. at the University of Genova reporting the selective functionalization of the 1,6-anhydro moiety and of the double bond of levoglucosenone #orgchem

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Synthesis of α-chloro-β-ketoesters via ytterbium(III) triflate-mediated decarboxylative Claisen-type condensation A Yb(OTf)3-mediated decarboxylative Claisen-type condensation is established to access α-chloro-β-ketoesters. Operating under mild conditions, this method delivers products in 78–95% yields while…

🔓Don't miss this #OpenAccess paper by Kazuaki Kudo et al. @utokyoofficial.bsky.social in our latest issue on the synthesis of α-chloro-β-ketoesters via ytterbium(iii) triflate-mediated decarboxylative Claisen-type condensation #orgchem

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Check out the research behind the cover from Nurettin Menges & co. at Necmettin Erbakan University reporting a gold(iii)-catalyzed Conia-ene reaction for the direct synthesis of substituted pyrroles from β-ketopropargyl amines #orgchem

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Enantioselective synthesis of antibiotic inducing gamma-butenolides from Streptomyces rochei and derivatives Given the challenges of discovering new natural products, further investigations into the regulatory systems that control their production are needed. Herein, we describe an enantioselective,…

🔓Read #OpenAccess research by Elizabeth Parkinson et al. at @purduechemistry.bsky.social in our latest issue describing the enantioselective synthesis of antibiotic inducing gamma-butenolides from Streptomyces rochei #orgchem #natprod

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Cell-penetrating peptides for therapeutic applications: emerging design strategies and future directions Cell-penetrating peptides (CPPs) are short amino acid sequences capable of traversing biological membranes and enabling intracellular delivery of diverse therapeutic cargos, thereby addressing core…

Don't miss in our latest issue this review dissecting the physicochemical design principles governing cell-penetrating peptide membrane interactions by Jiyoun Lee & co. at Sungshin Women's University #orgchem #medchem

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A supramolecular host with a cavitand core and four cholate side arms Copper(i)-catalyzed azide–alkyne cycloaddition (CuAAC) was employed to synthesize a new cavitand (1) having four cholate groups covalently connected to the cavitand core. CuAAC between a…

🔓Check out a #OpenAccess paper by Beijun Cheng, Angel E. Kaifer & co. @univmiami.bsky.social & Qilu University of Technology in our latest issue describing a supramolecular host with a cavitand core and four cholate side arms #orgchem

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Regioselective House–Meinwald rearrangement in oxindoles: access to substituted quinolinones House–Meinwald rearrangement of oxindole substrates facilitating a one-pot synthesis of 3-substituted 4-hydroxyquinolin-2-ones and quinoline-2,4-diones under EBHP and base-mediated conditions is…

Take a look in our latest issue at research from Sasidhar B. Somappa et al. reporting regioselective House–Meinwald rearrangement in oxindoles for access to substituted quinolinones #orgchem

📍CSIR-NIIST

Forcing the phenyl moiety into the axial position by embedding the 2-phenyl-1,3-dioxane system in a tricyclic benzomorphan scaffold: design, synthesis and biological evaluation The relative configuration and the substitution pattern control the interaction of 2-(2-phenyl1,3-dioxan-4-yl)ethan-1-amines with σ1 receptors or the PCP binding site of NMDA receptors. In order to…

🔓Be sure to read a #OpenAccess paper by Bernhard Wünsch & co. @uni-muenster.de in our latest issue embedding the 2-phenyl-1,3-dioxane system in a tricyclic benzomorphan scaffold to fix the phenyl moiety into the axial position #orgchem

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The Ugi–Joullié three-component reaction (UJ-3CR) and related reactions: recent developments, mechanistic aspects and synthesis of natural products and bioactive compounds The Ugi–Joullié three-component reaction evolved from the classic Ugi four-component reaction and enables the facile and efficient formation of polysubstituted nitrogen heterocycles from cyclic…

Don't miss this review in our latest issue by Teodoro Kaufman et al. from Universidad Nacional de Rosario looking at recent developments and mechanistic insights of the Ugi–Joullié three-component reaction #orgchem #natprod

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Check out the paper behind the cover from Guidong Lu, Minshou Wang, Shizhi Jiang & co. at Dali University describing the synthesis of a series of novel meroterpenoid natural products #orgchem #natprod

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DNA-based cooperative games: an interactive collective decision-making architecture Game theory provides an architecture for multi-agent strategic interactions, while DNA computing offers programmable, parallel molecular-scale operations, enabling unique “molecular gaming” systems…

Be sure to read research by Qiang Zhang & co. from Dalian University of Technology in our latest issue reporting a programmable majority-rule game-theoretic DNA based platform for molecular systems #orgchem

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Sustainable and green approaches for Knoevenagel condensation The Knoevenagel condensation reaction is one of the important and versatile transformations used to prepare a wide range of organic compounds bearing carbon–carbon double bonds. Therefore, it has…

Don't miss this review in our latest issue from Vinod Kumar et al. at Central University of Haryana summarising the recent developments in greener and sustainable synthetic approaches for Knoevenagel condensation #orgchem #greenchemistry

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TropMol: a cloud-based web tool for virtual screening and early-stage prediction of acetylcholinesterase inhibitors using machine learning Alzheimer's disease (AD) is the most common type of dementia, accounting for at least two-thirds of dementia cases in people aged 65 and older. Numerous approaches have been studied for the treatment…

Check out this paper by Thiago H. Doring at the Federal University of Santa Catarina describing a new cloud-based web tool for virtual screening and early-stage prediction of acetylcholinesterase inhibitors using machine learning #compchem #orgchem

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Take a look in our latest issue at a paper by Ahmad Takallou, Ahmed Al-Harrasi & co. describing how intramolecular hydrogen bonding in phenolic amides enables direct synthesis of indolizines #orgchem

📍University of Nizwa

Be sure to read research from Lin Dong et al. at Sichuan University in our latest issue reporting the synthesis and biological evaluation of fluorinated bergenin derivatives #orgchem

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🔓Don't miss this #OpenAccess review, part of our New Talent collection, in our latest issue by @syruegas.bsky.social & co. @yruegasgroup.bsky.social discussing recent advances of well-defined alkali metal complexes in organic synthesis #orgchem

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📢Our latest issue is now online!

Check out the paper behind the cover by Mattie Timmer, Bridget Stocker & co. @vicuniwgtn.bsky.social reporting the design & assessment of dimeric trehalose glycolipids to enhance Mincle-mediated vaccine adjuvanticity #medchem #orgchem

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Our postdoc Willi Amberg built SynStrategy, a learning tool that categorizes 500+ reactions by functional group with 400+ total synthesis examples. If you’re into #OrgChem, check it out (it’s free)!

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#ChemSky

Controlled packing of metal–peptide superhelices with β-peptide foldamers Metal–peptide superhelices formed from 12/10-helical β-peptide foldamers exhibit programmable hierarchical assembly. A single metal-coordinated superhelix organizes into distinct parallel or…

🔓Don't miss #OpenAccess research by Soo Hyuk Choi et al. from Yonsei University on the controlled packing of metal–peptide superhelices with β-peptide foldamers #orgchem #supramolecular

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