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Triazacryptand (TAC)-based fluorescent K sensors have broad biomedical utility, yet their advancement has been hindered because of their challenging synthesis. Herein, an efficient synthesis is reported that delivers a didesmethyl tri-azacryptand (ddTAC) K sensor in twofold fewer steps and ninefold higher overall yield than the original TAC synthesis. Our synthesis utilizes a C-O dianionic oxidative macrocyclization and reports new examples of aminoarylations and a microwave route to xanthythilium chromophores. The K sensitivity and selectivity of the ddTAC-based sensor are comparable to the TAC-based sensor.
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http://dx.doi.org/10.1002/ejoc.201001450 | DOI Listing |
J Agric Food Chem
September 2025
State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Structurally unique halichonine B is promising for the design of pharmaceutical leads, while function-oriented optimization is unknown in agrochemical science. Our recent practical synthesis offers a great chance for the discovery of antimicrobial leads. "Linker plus replaceable substituents" is exerted, in which up to 9 unique linkers together with diverse substituents from a wide chemical space are investigated for optimization of the readily available drimanyl amine.
View Article and Find Full Text PDFActa Crystallogr C Struct Chem
September 2025
College of Chemistry and Chemical Engineering, and Henan Key Laboratory of Function-Oriented Porous Materials, Luoyang Normal University, Luoyang, 471934, People's Republic of China.
Two 1:1 cocrystals of imidazo[1,2-a]pyridine-3-carbonitrile (IPC) with 4-nitrobenzoic acid (4-NBA) and 4-nitrophenol (4-NP), namely, imidazo[1,2-a]pyridine-3-carbonitrile-4-nitrobenzoic acid (1/1), CHN·CHNO or (IPC)·(4-NBA) (I), and imidazo[1,2-a]pyridine-3-carbonitrile-4-nitrophenol (1/1), CHN·CHNO or (IPC)·(4-NP) (II), were obtained and their crystal structures determined by single-crystal X-ray diffraction. Molecules of I and II are both linked by O-H..
View Article and Find Full Text PDFACS Med Chem Lett
August 2025
Department of Chemistry and Biochemistry, Loyola University Chicago, Chicago, Illinois 60660, United States.
The Hedgehog signaling pathway plays an essential role in cancer progression, including in basal cell carcinoma and medulloblastoma. This process is driven by oncogenic Gli transcription factors, which are regulated by the signaling protein Smoothened (Smo). While Smo inhibitors have shown clinical utility, drug resistance can limit their effectiveness.
View Article and Find Full Text PDFNat Prod Rep
August 2025
Department of Phytochemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, P. R. China.
Covering: 2013 to 2024Alkene-containing natural products (NPs) are abundantly present in plants, animals, and microorganisms. Strategic alkene modification of NPs not only generates diverse chemical libraries, enriching scaffold, stereochemistry and appendage variations but also aids in unraveling the intricate mechanisms and cellular targets of NPs. Over the past 15 years, visible-light photocatalysis and electrochemical catalysis have emerged as two highly promising approaches for novel chemical transformations.
View Article and Find Full Text PDFJ Org Chem
July 2025
College of Chemistry and Materials Engineering, Zhejiang A&F University, Hangzhou, Zhejiang 311300, P. R. China.
We have synthesized a series of sterically hindered ligands f-Amphbinol , which were successfully applied in the asymmetric hydrogenation of various ketones with excellent results (up to 63 examples, 95 → 99% yields, 90 → 99% ee, >20:1 dr). Ligand screening experiments demonstrated that the enantioselectivity of hydrogenation increases with the increase in the steric hindrance of substituents on P-aryl rings of the ligand. Besides, the key intermediates for API Ladostigil were successfully synthesized with this catalyst system, which hinted at the potential applications.
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