Herein, we introduce an efficient and straightforward strategy for the selective C-H esterification and alkylation of quinoxalin-2(1)-ones with aldehydes. A key feature of our study is the ability to perform both C-H esterification and alkylation using different types of aldehydes. The reaction system is highly compatible with a range of quinoxalin-2(1)-ones and aldehydes, yielding C3-esterified and C3-alkylated products in moderate-to-good yields. The applicability of this approach is further enhanced by its scalability through continuous-flow synthesis, late-stage modification of significant molecules, and product derivatization. Our mechanistic investigations reveal a radical relay mechanism, triggered by a hydrogen atom transfer process.
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http://dx.doi.org/10.1021/acs.orglett.5c00631 | DOI Listing |
Fitoterapia
March 2025
College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China; Department of Marine Biopharmacology, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China; Marine Biomedical Science and Technology Innovation Platform of Lin-gang Special Area, Shanghai 201306, China. Electronic address:
A series of novel demethylzeylasteral derivatives 1-3 was synthesized by performing modifications on the aldehyde groups at the C-4 positions. Subsequently, the anti - proliferative activities of derivatives 1-3 was evaluated using three human cancer cell line models (HCT116, SKOV3, and HepG2) and the CCK - 8 assay. Compared with demethylzeylasteral, derivative 2 exhibited a remarkable inhibitory effect on HCT116 (4.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
March 2025
Laboratório de Tecnologia e Desenvolvimento de Compósitos e Materiais Poliméricos (LaCoPol), Universidade Federal de Pelotas (UFPel), Campus Capão do Leão s/n, Pelotas, RS 96010-900, Brazil. Electronic address:
Atopic dermatitis (AD) is a chronic disorder affecting millions worldwide. Recent advancements suggest that combining therapies can significantly improve AD treatment outcomes and mitigate the challenges of long-term drug use, particularly with corticosteroids. In this study, we developed a 3D-printed hydrogel composed of gelatin (Gel) and dialdehyde starch (DAS), capable of encapsulating and delivering hydrocortisone (HC).
View Article and Find Full Text PDFOrg Biomol Chem
March 2025
National & Local Joint Engineering Research Center for Mineral Salt Deep Utilization, Huaiyin Institute of Technology, Huaian 223003, China.
A novel, efficient and sustainable methodology involving visible-light-mediated construction of pyrazolo[4,3-]pyrimidin-7(6)-ones from easily available 4-amino-1-methyl-3-propyl-1-pyrazole-5-carboxamide and aldehydes in the presence of 4CzIPN under an oxygen atmosphere has been developed. This photocatalytic system worked under mild conditions and avoided the use of any excess amount of toxic oxidants and transition metals. A variety of functionalized products were obtained in good to excellent yields.
View Article and Find Full Text PDFEnviron Geochem Health
March 2025
Institute of Soil Fertilizer and Agricultural Water Saving, Xinjiang Academy of Agricultural Sciences, Urumqi, 830091, People's Republic of China.
Microplastics (MPs), as a global environmental issue, have unclear impacts on agricultural ecosystems. Cotton, as a major agricultural crop in Xinjiang, requires plastic film covering to ensure its yield. The widespread use of plastic film (commonly made of polyethylene) in cotton cultivation has led to significant concerns about microplastic pollution in cotton fields.
View Article and Find Full Text PDFDiabetologia
March 2025
Department of Endocrinology and Metabolism, Zhongshan Hospital, Fudan University, Shanghai, China.
Aims/hypothesis: Fat deposition in the pancreas is implicated in beta cell dysfunction and the progress of type 2 diabetes. However, there is limited evidence to confirm the correlation and explore how pancreatic fat links with beta cell dysfunction in human type 2 diabetes. This study aimed to examine the spatial relationship between pancreatic fat and islets in human pancreases.
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