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1000 results for “organic_chemistry”
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Joseph Tuccinardi and John Wood from Baylor University (#USA), introduced a novel strategy to efficiently synthesize the core scaffold of aleutianamine. Their study involved a vinylogous Mukaiyama-Michael reaction cascade using two previously unknown coupling partners. Published in #JACS
https://me.organicchemistry.eu/post/aleutianamine-jacs-2025/
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Joseph Tuccinardi and John Wood from Baylor University (#USA), introduced a novel strategy to efficiently synthesize the core scaffold of aleutianamine. Their study involved a vinylogous Mukaiyama-Michael reaction cascade using two previously unknown coupling partners. Published in #JACS
https://me.organicchemistry.eu/post/aleutianamine-jacs-2025/
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Computer-aided synthesis: R. Shenvi and C. Li published in #Nature the total synthesis of 25 picrotoxanes. Their 1,5-HAT key reaction was challenged by β-scission, therefore DFT based calculations helped to design usable intermediates.
Read more on my page: https://me.organicchemistry.eu/post/picrotoxanes-nature-2024/
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Another total synthesis in the spotlight: Already early this year Mingji Dai and his research team described the total synthesis of heilonine in #JACS (doi: 10.1021/jacs.3c13492). This synthesis is short and elegant, using multiple C-H functionalisations and a Nazarov cyclisation for their key step.
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Another total synthesis in the spotlight: Already early this year Mingji Dai and his research team described the total synthesis of heilonine in #JACS (doi: 10.1021/jacs.3c13492). This synthesis is short and elegant, using multiple C-H functionalisations and a Nazarov cyclisation for their key step.
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Another total synthesis in the spotlight: Already early this year Mingji Dai and his research team described the total synthesis of heilonine in #JACS (doi: 10.1021/jacs.3c13492). This synthesis is short and elegant, using multiple C-H functionalisations and a Nazarov cyclisation for their key step.
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Another total synthesis in the spotlight: Already early this year Mingji Dai and his research team described the total synthesis of heilonine in #JACS (doi: 10.1021/jacs.3c13492). This synthesis is short and elegant, using multiple C-H functionalisations and a Nazarov cyclisation for their key step.
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Another total synthesis in the spotlight: Already early this year Mingji Dai and his research team described the total synthesis of heilonine in #JACS (doi: 10.1021/jacs.3c13492). This synthesis is short and elegant, using multiple C-H functionalisations and a Nazarov cyclisation for their key step.
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Total Synthesis of Pleurotin (JACS Au, Y. Q. Long 2024)
Pleurotin is a benzoquinone meroterpenoid that was first isolated in the late 1940s. Since that time, several total syntheses of this compound have been reported. Recently, Ya-Qiu Long and his team from Soochow University (#China) published a novel synthetic route in the journal JACS Au.
Read more here: https://www.organicchemistry.eu/books/total-syntheses-of-natural-products/page/total-synthesis-of-pleurotin-y-q-long-2024
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Efficient Synthesis of ProTide antivirals: A team from from #Fudan University and #Shanghai Jiao Tong University reporting a copper-catalyzed method for synthesizing chiral phosphates in #JACS.
This research represents a new tool for the synthesis of ProTide nucleoside analogues, providing an efficient route that can enhance the development of antiviral drugs in future studies.
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Efficient Synthesis of ProTide antivirals: A team from from #Fudan University and #Shanghai Jiao Tong University reporting a copper-catalyzed method for synthesizing chiral phosphates in #JACS.
This research represents a new tool for the synthesis of ProTide nucleoside analogues, providing an efficient route that can enhance the development of antiviral drugs in future studies.
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Efficient Synthesis of ProTide antivirals: A team from from #Fudan University and #Shanghai Jiao Tong University reporting a copper-catalyzed method for synthesizing chiral phosphates in #JACS.
This research represents a new tool for the synthesis of ProTide nucleoside analogues, providing an efficient route that can enhance the development of antiviral drugs in future studies.
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Efficient Synthesis of ProTide antivirals: A team from from #Fudan University and #Shanghai Jiao Tong University reporting a copper-catalyzed method for synthesizing chiral phosphates in #JACS.
This research represents a new tool for the synthesis of ProTide nucleoside analogues, providing an efficient route that can enhance the development of antiviral drugs in future studies.
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Efficient Synthesis of ProTide antivirals: A team from from #Fudan University and #Shanghai Jiao Tong University reporting a copper-catalyzed method for synthesizing chiral phosphates in #JACS.
This research represents a new tool for the synthesis of ProTide nucleoside analogues, providing an efficient route that can enhance the development of antiviral drugs in future studies.
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The construction of quaternary centres via C-C bond formation is a major challenge. A new stereoselective method using lithium enolates and Ru-catalysed allylic substitution has been reported in #JACS by the group of Erick Carreira (ETH #Zürich). This promising approach provides access to these sterically crowded motifs.
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The construction of quaternary centres via C-C bond formation is a major challenge. A new stereoselective method using lithium enolates and Ru-catalysed allylic substitution has been reported in #JACS by the group of Erick Carreira (ETH #Zürich). This promising approach provides access to these sterically crowded motifs.
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The construction of quaternary centres via C-C bond formation is a major challenge. A new stereoselective method using lithium enolates and Ru-catalysed allylic substitution has been reported in #JACS by the group of Erick Carreira (ETH #Zürich). This promising approach provides access to these sterically crowded motifs.
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The construction of quaternary centres via C-C bond formation is a major challenge. A new stereoselective method using lithium enolates and Ru-catalysed allylic substitution has been reported in #JACS by the group of Erick Carreira (ETH #Zürich). This promising approach provides access to these sterically crowded motifs.
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The construction of quaternary centres via C-C bond formation is a major challenge. A new stereoselective method using lithium enolates and Ru-catalysed allylic substitution has been reported in #JACS by the group of Erick Carreira (ETH #Zürich). This promising approach provides access to these sterically crowded motifs.
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The synthesis of #drug libraries is key in drug discovery but can be inefficient, especially in small labs. Jiang Weng and colleagues at Sun Yat-Sen University (#Guangzhou #China) propose a reagent-free sulfamide coupling strategy to form bifunctional molecules. This method allows the coupling of acid and amine on a 96-well plate without additives published in the journal Angewandte Chemie.
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Stasseriolides are a class of polyketide natural products with interesting biological activities, but they are limited in natural abundance. A recent synthesis of stasseriolides A-D by Alois Fürstner's group at the Max Planck Institute für Kohlenforschung reported in Angewandte Chemie employed ring-closing alkyne metathesis, providing access to the natural products and enabling the preparation of analogues.
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Researchers from the Keele University and TU #Berlin have developed a biocatalytic method to diversify thionucleosides, demonstrating that enzyme-catalyzed transglycosylation can effectively facilitate nucleobase exchange and applied this technique to synthesize 5-ethynyl-4'-thiouridine for cellular labeling using click chemistry. Published in #AngewandteChemie
https://onlinelibrary.wiley.com/doi/full/10.1002/anie.202405040
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Remdesivir, a successful #antiviral for #COVID19 inspired a new nucleoside analogue with a CN group at the 4' position, exhibiting broad-spectrum activity against RSV, pneumo- and picornaviruses. This analogue demonstrates promising cellular uptake, triphosphate formation, and efficacy in respiratory tissues, with a possibility of an inhaled treatment. Published by #Gilead #Science in #biorxiv
#chemistry #drug #MedicinalChemistry
https://www.biorxiv.org/content/10.1101/2024.04.17.589937v1.full
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Structural Modifications Enhance Antibacterial Potency of Bacitracin
The team of N. Martin from Leiden University optimized the antibiotic bacitracin, leading to a 256-fold increase in activity and also showed activity against vancomycin-resistant strains.
The team made the compound's non-polar side chains more lipophilic, enhancing bacterial membrane anchoring and hydrophobic interactions.
#MedicinalChemistry #Chemistry #Science #Research
Read more in #PNAS: https://www.pnas.org/doi/10.1073/pnas.2315310121
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Terpenoids are a large class of secondary #NaturalProducts, with some possessing an interesting polycyclic core that has attracted research interest. Researchers from #Shandong #University in #China led by Ze-Jun Xu (徐泽军) and Hong-Xiang Luo (娄红祥) have now reported the #TotalSynthesis of platensilin and platensimycin, as well as the formal synthesis of platencin, using a biomimetic approach from a common precursor.
Read more in #JACS: https://pubs.acs.org/doi/10.1021/jacs.4c02256
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My Reading Tip of the Week:
Scabrolide A, a polycyclic marine natural product, has fascinated chemists due to its highly constrained structure. Recently, Pengfei Hu and colleagues from Westlake University in Hangzhou, China, published an innovative radical cascade strategy for efficiently synthesizing the scaffold of this polycyclic compound.
Divergent Synthesis of Scabrolide A and Havellockate via an exo-exo-endo Radical Cascade
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Synthesis of Polysubstituted Bicyclo[1.1.0]butanes by Ilan Marek (#Israel Institute of Technology) published in #JACS
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Researchers (Rahul Choudhury et al.) from the Academy of Scientific and Innovative Research in #India reported in the journal #OrganicLetters the total synthesis of benzo[g]isochromene stereodiads. Their synthesis using a TiCl4 promoted #Aldol coupling showed that the previously reported absolute structure did not agree with the structure of the natural product and a revision was suggested.
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Melognine was thought to be a highly complex alkaloid with a polycyclic ring system. Yui Irie and Satoshi Yokoshima (Nagoya University, #Japan) published a total synthesis of the proposed structure in the journal #JACS. However, the synthesised structure turned out to have different analytical properties. The authors concluded that melognine is actually identical to melodinine L. Check out the intriguing total synthesis route on JACS:
https://pubs.acs.org/doi/10.1021/jacs.4c02086 -
If you have some time, take a look at the total synthesis of Hunterine A by Elliot Hicks, Kengo Inoue and Brian Stoltz published in #JACS (#OpenAccess). Very elegant synthesis and late-stage cyclization strategy.