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We report the direct asymmetric synthesis of pyrimido[2,1-]benzothiazoles using a commercially available chiral amine catalyst. A variety of 2-benzothiazolimines and aldehydes were well tolerated under the reaction conditions and generated the corresponding products in 81-99% yields with excellent diastereoselectivities and enantioselectivities (up to >20:1 dr, 99% ee). Furthermore, the products could be easily converted to other useful chiral building blocks.
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http://dx.doi.org/10.1021/acs.joc.0c02499 | DOI Listing |
J Agric Food Chem
September 2025
School of Science, Asymmetric Synthesis and Chirotechnology Key Laboratory of Sichuan Province, Xihua University, Chengdu 610039, P. R. China.
The emergence of severe resistance issues in plant pathogenic fungi poses a significant threat to the global quality and safety of crops. In this study, 36 novel derivatives featuring a 5,6,7,8-tetrahydroquinazolin structure were designed and synthesized for the first time. These 36 target compounds were subjected to tests against five fungal species.
View Article and Find Full Text PDFSmall
September 2025
College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University, Jinan, 250014, P. R. China.
The functionality of covalent organic frameworks (COFs) is usually highly related to their morphologies. Among various morphologies, the hollow-structured COFs have recently attracted intense attention due to their unique properties. Herein, the synthesis of hollow structured COFs are first reported with the chiral internal sites via combining the chiral templating method with the acid etching approach.
View Article and Find Full Text PDFEur J Case Rep Intern Med
August 2025
General medicine department, Universidad de Cartagena, Cartagena, Colombia.
Background: Romosozumab is a sclerostin-inhibiting monoclonal antibody that is effective and safe for anabolic treatment in patients with osteoporosis. Its main adverse effects are local; the severity of these injection-site reactions in clinical trials was generally mild.
Case Report: We present a case of a 71-year-old Colombian woman with osteoporosis at very high risk of fractures with no relevant history of drug allergies.
Beilstein J Org Chem
August 2025
Department of Natural Sciences and Sustainable Resources, Institute of Organic Chemistry, BOKU University, 1190 Vienna, Austria.
Nonreducing disaccharides are prevalent in non-mammalian glycans and glycolipids, serving as pivotal structural components in mycobacterial glycans, microbial oligosaccharide and nucleoside antibiotics, as well as biologically active mimetics of bacterial pathogen-associated molecular patterns (PAMPs). As integral components of PAMPs, 1,1'-linked disaccharide-containing biomolecules play important roles in host-pathogen interactions, cellular signaling, and pathogenesis. Accessing complex biomolecules containing nonreducing disaccharides is often hindered by difficulties in isolating them from natural sources, which can result in impure or degraded products, particularly when sensitive functional groups are involved.
View Article and Find Full Text PDFBeilstein J Org Chem
September 2025
State Key Laboratory of Chemical Resource Engineering, Department of Organic Chemistry, College of Chemistry, Beijing University of Chemical Technology, Beijing 100029, People's Republic of China.
Both chiral bisoxazolines and bisimidazolines are efficient chiral ligands in metal-catalyzed asymmetric organic transformations. Chiral cyclohexane-linked bisimidazolines were prepared from optically active cyclohexane-1,2-dicarboxylic acid and 1,2-diphenylethane-1,2-diamines via the monosulfonylation of 1,2-diphenylethane-1,2-diamines, condensation of -sulfonylated 1,2-diphenylethane-1,2-diamines and cyclohexane-1,2-dicarboxylic acid, and the final cyclization with the in situ generated Hendrickson reagent.
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