Org Lett
Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen 518055, China.
Published: November 2008
We reported herein a diversity-oriented synthesis of a range of fused pyran-gamma-lactones that was effected through a versatile Pd-thiourea complex-catalyzed intramolecular alkoxycarbonylative annulation.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1021/ol802115u | DOI Listing |
Org Lett
February 2025
National Engineering Research Center for Carbohydrate Synthesis, Jiangxi Province Key Laboratory of Natural and Biomimetic Drugs Research, College of Chemistry and Materials, Jiangxi Normal University, Nanchang, Jiangxi 330022, China.
A rhodium-catalyzed annulation of 2-azirines with enaminones is presented. This protocol affords a convenient approach to the diversity-oriented synthesis of 4-acyl- and 4-formyl pyrroles with good functional group tolerance. The utility of this reaction has been demonstrated by scale-up preparation, late-stage modification of natural molecules, and synthesis of diverse derivatives.
View Article and Find Full Text PDFEur J Med Chem
April 2025
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute BS, 10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India; Sophisticated Analytical Instrument Facility & Research, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, Uttar Pradesh, India. Electronic address:
A library of 30 novel quinazolinone-dihydropyrimidinone derivatives was synthesized employing a diversity-oriented approach for the identification of potential anti-diabetic therapeutic lead. In vitro evaluation revealed that seven compounds (5d, 5e, 5i, 5j, 5l, 5m and 5s) significantly enhanced the rate of GLUT4 translocation to the cell surface in L6-GLUT4myc myotubes. Out of these, compound, 5m exhibited promising potency to stimulate GLUT4 translocation in skeletal muscle cells via activating AMPK-dependent pathway, but independent to PI-3-K/AKT signaling.
View Article and Find Full Text PDFJ Org Chem
February 2025
Syngenta Biosciences Private Limited, Santa Monica Works, Corlim 403110, Goa, India.
We report the first total synthesis of -8-deoxoantidesmone and -waltherione M, key intermediates in the unexplored 5,6,7,8-tetrahydro-1H-quinolin-4-one waltherione (THQW) alkaloid family. These compounds have been synthesized in three steps via a diversity-oriented approach utilizing a versatile intermediate 8-bromo-5-fluoro-3-methoxy-2-methyl-1H-quinolin-4-one, which was obtained through a one-step synthesis between 2-bromo-5-fluoro-aniline and ethyl 2-methoxy-3-oxo-butanoate. This intermediate underwent a MgCl-mediated SAr reaction using alkyl Grignard reagents to provide 8-bromo-3-methoxy-2-methyl-5-alkyl-1H-quinolin-4-one.
View Article and Find Full Text PDFNat Commun
January 2025
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.
Stereocontrolled construction of tetrasubstituted olefins has been an attractive issue yet remains challenging for synthetic chemists. In this manuscript, alkynyl selenides, when treated with ArBCl, are subject to an exclusive 1,1-carboboration, affording tetrasubstituted alkenes with excellent levels of E-selectivity. Detailed mechanistic studies, supported by DFT calculations, elucidates the role of selenium in this 1,1-addition process.
View Article and Find Full Text PDFChemMedChem
January 2025
Departamento de Química Orgánica, Instituto de Química, Universidad Nacional Autónoma de México (UNAM), CDMX, México.
A diversity-oriented collection of furan-2-carboxamides with antibiofilm activity against P. aeruginosa is reported. The design involved the bioisosteric replacement of the labile furanone ring by a furan-2-carboxamide moiety to explore its influence on biological activity.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!
© LitMetric 2025. All rights reserved.