A novel method has been developed for the synthesis of 1,3-thiazin-4-one compounds containing trifluoromethyl groups utilizing 2-trifluoromethyl acrylic acid and thioamides as key starting materials. This protocol is characterized by its simplicity, practicality, and tolerance toward various functional groups. Given the straightforward nature of the procedure, the ready availability of both starting materials, and the significance of drugs containing trifluoromethyl, it is anticipated that this reaction will have wide-ranging applications.
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http://dx.doi.org/10.1021/acs.joc.4c01310 | DOI Listing |
Research (Wash D C)
December 2024
College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou, Zhejiang 325035, China.
Photoelectrochemistry provides an important application in the production of high-value-added chemicals. However, photoelectrochemical organic transformation with high product selectivity remains a challenge. Until now, various technologies have been developed to promote the selectivity of photoelectrochemical high-value-added chemical production.
View Article and Find Full Text PDFChem Biodivers
December 2024
Guizhou Medical University, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Science City,Baiyun District,Guiyang, 550014, Guiyang, CHINA.
A series of Matijin-Su (MTS) derivatives were designed, synthesized and the anti-HBV activity evaluated in vitro. Twelve compounds displayed good inhibition on HBV DNA replication with micromolar IC50 values (0.14 - 4.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, Taiwan; School of Pharmacy, Taipei Medical University, Taipei, Taiwan. Electronic address:
Protein disulfide isomerase (PDI) regulates multiple protein functions by catalyzing the oxidation, reduction, and isomerization of disulfide bonds. The enzyme is considered a potential target for treating thrombosis. We previously developed a potent PDI inhibitor, CPD, which contains the propiolamide as a warhead targeting cysteine residue in PDI.
View Article and Find Full Text PDFJ Pharmacol Sci
January 2025
Department of Pathological and Molecular Pharmacology, Faculty of Pharmacy, Osaka Medical and Pharmaceutical University, Takatsuki, Osaka, 569-1094, Japan.
Nitric oxide (NO)-donor drugs, which stimulate reduced form of soluble guanylate cyclase (sGC), have different efficacy to the arteries and veins. This study examined whether sGC activators, which activate oxidized/apo sGC, also have arteriovenous selectivity similar to that of NO-donor drugs. The mechanical responses of the isolated blood vessels were assessed using the organ chamber technique and protein expression was verified using western blotting.
View Article and Find Full Text PDFChem Commun (Camb)
December 2024
Graduate School of Science and Engineering, Yamaguchi University, 2-16-1 Tokiwadai, Ube, Yamaguchi, 755-8611, Japan.
The introduction of multiple trifluoromethyl (CF) groups into aromatic compounds remains a significant challenge in synthetic chemistry. Here, we report an unprecedented visible light-promoted multiple trifluoromethylation of phenols using commercially available CFI. The key to success lies in our discovery of a "continuous activation strategy" that enables sequential trifluoromethylations through single-electron transfer from photoexcited phenoxide to CFI until all or positions are occupied.
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