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Herein, for the first time, the controllable, accurate, and diverse synthesis of all ring sizes of medium-sized (8- to 11-membered) indole-derived bridged biaryls has been realized by using ingeniously designed -alkynylnaphthols that feature cyclic amines with adjustable ring sizes. The transformation may proceed through a DBN-mediated in-situ generation of vinylidene -quinone methides/indole-ring formation/ring expansion cascade sequence, which is characterized by acceptable to excellent yields and good functional group tolerance.
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http://dx.doi.org/10.1021/acs.orglett.5c00531 | DOI Listing |
Beilstein J Org Chem
August 2025
Faculty of Chemistry (Organic Chemistry) and Center for Nanointegration Duisburg-Essen (CENIDE), University of Duisburg-Essen, 45141 Essen, Germany.
Chiral macrocycles hold significant importance in various scientific fields due to their unique structural and chemical properties. By controlling their size, shape, and substituents, chiral macrocycles offer a platform for designing and synthesizing highly efficient catalysts, chemosensors, and functional materials. We have recently made strides in developing macrocyclic organocatalysts; however, their synthesis remains challenging.
View Article and Find Full Text PDFJ Int Assoc Provid AIDS Care
September 2025
Department of Internal medicine, School of Medicine, College of Medicine and Health Sciences, University of Gondar, Gondar, Ethiopia.
BackgroundDolutegravir (DTG)-based antiretroviral treatment is now the recommended regimen because of its high efficacy and fewer adverse effects. Nonetheless, hyperglycemia as adverse effect of DTG was reported in few clinical observations.MethodsA case-control study was carried out among DTG-based antiretroviral therapy (ART) users during the study period.
View Article and Find Full Text PDFPhys Med Biol
September 2025
State Key Laboratory of Nuclear Physics and Technology, and Key Laboratory of HEDP of the Ministry of Education, CAPT, Peking University, Beijing 100871, China, Beijing, Beijing, 100871, CHINA.
The development of FLASH radiotherapy (FLASH-RT) is limited by the availability of ultra-high dose rate (UHDR) irradiation platform. This study aims to optimize electron scattering foils (SFs) for a compact 6 MeV linear accelerator (linac) operating at a short source-to-surface distance (SSD), enabling lateral uniform dose delivery with UHDR for FLASH-RT studies. Approach: Based on a custom-built linac, optimized aluminum SFs were designed using the Nelder-Mead simplex algorithm coupled with Geant4 Monte-Carlo simulations to achieve lateral dose uniformity in 10 mm of water/PMMA below the surface at a reduced SSD.
View Article and Find Full Text PDFChem
August 2025
Department of Chemistry, The University of Chicago, Chicago, IL 60637, USA.
Ring-contraction reactions are valuable transformations to access harder-to-synthesize smaller-sized rings from more available larger-sized precursors. Herein, we report an unprecedented lactam downsizing strategy by taking advantage of removable directing groups (DGs) and Rh-catalyzed C-C activation. An efficient method for DG installation to common lactam substrates is developed by employing silylated amines and Ti catalysts, and the resulting amidine moiety can be converted back to lactams via acid-mediated hydrolysis.
View Article and Find Full Text PDFOrg Lett
September 2025
Institute of Chemistry, Casali Center of Applied Chemistry, The Hebrew University of Jerusalem, Jerusalem 9190401, Israel.
We report a selective dearomative cyclization strategy for the synthesis of 3,4-fused diazabicycles from 3-substituted pyridyl ynamides. The method combines a chemo-, regio-, and stereoselective carbometalation with a regioselective dearomatization, enabling access to a broad range of diazabicyclic scaffolds with varied ring sizes. The protocol accommodates alkyl and aryl Grignard reagents, tolerates diverse functional groups, and supports stereodivergent synthesis, offering a versatile platform for constructing complex fused -heterocycles with potential relevance to medicinal chemistry.
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