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1000 results for “organic_chemistry”
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PKMYT1 is a promising target for #cancer #drug developmenent. While some inhibitors such as RP-6036 are available for some time, researchers from InSilico #Medicine have now introduced a novel #PROTAC degrader based on their computational design of a novel inhibitor. This study was now published in #Nature Communications (2025):
https://www.nature.com/articles/s41467-025-65796-8#drugdesign #chemistry #MedicinalChemistry #research #science
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PKMYT1 is a promising target for #cancer #drug developmenent. While some inhibitors such as RP-6036 are available for some time, researchers from InSilico #Medicine have now introduced a novel #PROTAC degrader based on their computational design of a novel inhibitor. This study was now published in #Nature Communications (2025):
https://www.nature.com/articles/s41467-025-65796-8#drugdesign #chemistry #MedicinalChemistry #research #science
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PKMYT1 is a promising target for #cancer #drug developmenent. While some inhibitors such as RP-6036 are available for some time, researchers from InSilico #Medicine have now introduced a novel #PROTAC degrader based on their computational design of a novel inhibitor. This study was now published in #Nature Communications (2025):
https://www.nature.com/articles/s41467-025-65796-8#drugdesign #chemistry #MedicinalChemistry #research #science
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PKMYT1 is a promising target for #cancer #drug developmenent. While some inhibitors such as RP-6036 are available for some time, researchers from InSilico #Medicine have now introduced a novel #PROTAC degrader based on their computational design of a novel inhibitor. This study was now published in #Nature Communications (2025):
https://www.nature.com/articles/s41467-025-65796-8#drugdesign #chemistry #MedicinalChemistry #research #science
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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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⚗️ For everyone interested in the synthesis of #antiviral #drugs:
I collected 7 synthesis routes for #entecavir, a marketed #HBV antiviral. At first sight, this carbocyclic nucleoside analogue looks quite simple, however, its synthesis requires a multi-step total synthesis.
Check the article for further information and share it with your audience:
https://www.organicchemistry.eu/books/nucleoside-analogues/page/synthesis-strategies-for-entecavir
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⚗️ For everyone interested in the synthesis of #antiviral #drugs:
I collected 7 synthesis routes for #entecavir, a marketed #HBV antiviral. At first sight, this carbocyclic nucleoside analogue looks quite simple, however, its synthesis requires a multi-step total synthesis.
Check the article for further information and share it with your audience:
https://www.organicchemistry.eu/books/nucleoside-analogues/page/synthesis-strategies-for-entecavir
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⚗️ For everyone interested in the synthesis of #antiviral #drugs:
I collected 7 synthesis routes for #entecavir, a marketed #HBV antiviral. At first sight, this carbocyclic nucleoside analogue looks quite simple, however, its synthesis requires a multi-step total synthesis.
Check the article for further information and share it with your audience:
https://www.organicchemistry.eu/books/nucleoside-analogues/page/synthesis-strategies-for-entecavir
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⚗️ For everyone interested in the synthesis of #antiviral #drugs:
I collected 7 synthesis routes for #entecavir, a marketed #HBV antiviral. At first sight, this carbocyclic nucleoside analogue looks quite simple, however, its synthesis requires a multi-step total synthesis.
Check the article for further information and share it with your audience:
https://www.organicchemistry.eu/books/nucleoside-analogues/page/synthesis-strategies-for-entecavir
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⚗️ For everyone interested in the synthesis of #antiviral #drugs:
I collected 7 synthesis routes for #entecavir, a marketed #HBV antiviral. At first sight, this carbocyclic nucleoside analogue looks quite simple, however, its synthesis requires a multi-step total synthesis.
Check the article for further information and share it with your audience:
https://www.organicchemistry.eu/books/nucleoside-analogues/page/synthesis-strategies-for-entecavir
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Total synthesis of periglaucine C and other hasubanan alkaloids. The Shuanhu Gao Group from the East China Normal University (Shanghai) published in the journal Angewandte Chemie the synthesis of these natural products featuring an intramolecular Diels Alder reaction after photoenolization and a late stage Michael addition.
https://onlinelibrary.wiley.com/doi/epdf/10.1002/anie.202214873
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A novel bifunctional molecule induces selective nitrosation of BTK. Mechanistically, it first covalent bind to BTK and the release NO, which yielded in the nitrosation of a cysteine side chain. Published in #JACS by Jiangbing Wu, Zhangjian Huang and coworkers (#China)
Read more on doi: 10.1021/jacs.5c07409 or on my page: https://me.organicchemistry.eu/post/nitrosation-jacs-2025/
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When you think of a reaction between an acid and an alcohol, you think of an ester as the product. MacMillan and co-workers from Princeton have now described a different pathway: Selective decarbonylative C-C coupling via a metal-catalyzed photoredox reaction. Read more about this in JACS:
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Novel enantioselective #synthesis of rubriflordilactone B by Gui and colleagues from the Chinese Academy of Science published in #JACS
This is already the second total synthesis of this group, with an interesting reaction cascade as the key reaction in this process. -
Luo et al. from Tsinghua University (#China) report in #JACS a novel method to create enantioenriched α-amino aldehydes using a chiral amine catalyst and iridium photocatalysis. Through this strategy α-amino aldehydes with up to 93% ee could be synthesised and subsequently stabilised via analogues formation (e.g. through Wittig reaction).
https://me.organicchemistry.eu/post/deracemization-aldehyde-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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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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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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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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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.
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The #TotalSynthesis of highly condensed polycyclic terpenoids has been a hot topic in #Chemistry recently. Yandong Zhang (#Xiamen University, #China) and co-workers now were able to synthesize such complex terpenes by epoxide-ene cyclization, oxygenation, and subsequent skeletal rearrangement. Read more about this protecting group free total synthesis in #JACS: https://pubs.acs.org/doi/10.1021/jacs.3c06442
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Synthesis of highly complex terpenoids reported by Shuanhu Gao and co-workers from the East China Normal #University (#Shanghai #China). Cephinoid P and other related terpenoids were accessible by Nicholas/Hosomi-Sakurai cascade reaction and Pauson-Khand reaction. Published in #JACS
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⚗️ #TotalSynthesis of Waixenicin A, 9-Deacetoxy-14,15-deepoxyxeniculin and Xeniafaraunol A by Thomas Magauer and colleagues (#University of #Innsbruck @uniinnsbruck #Austria) published recently in #JACS featuring an unusual alkylation ring closing strategy.
#chemistry #organicchemistry @chemistry
📰 https://pubs.acs.org/doi/10.1021/jacs.3c03366 -
The beauty of spirocyclic compounds: Total synthesis of illisimonin A by Markus Kalesse and co-workers from the University Hannover published recently in #JACS
Nazarov/ene cyclization lead to key intermediate for the #synthesis of this terpenoid.
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Stephadiamine is a popular synthetic challenge which resulted in many total syntheses before. Now, Jieping Zhu (EPFL, Lausanne) and co-workers were able to report in #JACS a new route to the #alkaloid with a hasubanan core structure featuring a diastereoselective intramolecular dipolar cycloaddition.
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"Z-Trisubstituted α,β-Unsaturated Esters and Acid Fluorides through Stereocontrolled Catalytic Cross-Metathesis" published in #JACS by Hoveyda and co-workers (Boston College, #USA).
#chemistry #orgchem @chemistry
https://pubs.acs.org/doi/10.1021/jacs.2c13245 -
Nowadays, a lot of total #synthesis projects include terpenes with a C-H functionalization strategy.
In contrast, Alois Fürstner and co-workers (MPG Mülheim) recently presented their synthesis of prorocentin, a complex #polyketide, in #JACS featuring up-to-date transformations and beautifully designed synthetic routes. I added this synthesis now to my collection, have a look 👇