An increased supply of scarce or inaccessible natural products is essential for the development of more sophisticated pharmaceutical agents and biological tools, and thus the development of atom-economical, step-economical and scalable processes to access these natural products is in high demand. Herein we report the development of a short, scalable total synthesis of (-)-α-kainic acid, a useful compound in neuropharmacology that is, however, limited in supply from natural resources. The synthesis features sequential platinum-catalyzed direct allylic aminations and thermal ene-cyclization, enabling the gram-scale synthesis of (-)-α-kainic acid in six steps and 34% overall yield.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/chem.201406557 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Metabolic dysfunction associated steatotic liver and kidney stones: what is going on?
Curr Opin Nephrol Hypertens
January 2025
Department of Urology, University of Alabama at Birmingham, Birmingham, Alabama, USA.
Purpose Of Review: Metabolic dysfunction associated steatotic liver disease (MASLD) is increasing throughout the world, affecting nearly one in three individuals. Kidney stone disease, which is also increasing, is associated with MASLD. Common risk factors for both, including obesity, diabetes, dyslipidemia, hypertension, and metabolic syndrome, are likely drivers of this association.
View Article and Find Full Text PDFKaMLs for Predicting Protein p Values and Ionization States: Are Trees All You Need?
J Chem Theory Comput
January 2025
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201, United States.
Despite its importance in understanding biology and computer-aided drug discovery, the accurate prediction of protein ionization states remains a formidable challenge. Physics-based approaches struggle to capture the small, competing contributions in the complex protein environment, while machine learning (ML) is hampered by the scarcity of experimental data. Here, we report the development of p ML (KaML) models based on decision trees and graph attention networks (GAT), exploiting physicochemical understanding and a new experiment p database (PKAD-3) enriched with highly shifted p's.
View Article and Find Full Text PDFUltra-Early Hematoma Expansion Is Associated With Ongoing Hematoma Growth and Poor Functional Outcome.
Stroke
January 2025
Departments of Medicine and Neurology, Melbourne Brain Centre @ The Royal Melbourne Hospital, University of Melbourne, AUSTRALIA.
There is limited data on ultra-early hematoma growth dynamics and its clinical relevance in primary intracerebral hemorrhage (ICH). We aimed to estimate the incidence of hematoma expansion (HE) within the hyperacute period of ICH, describe hematoma dynamics over time, investigate the associations between ultra-early HE and clinical outcomes after ICH, and assess the effect of tranexamic acid on ultra-early HE. We performed a planned secondary analysis of the STOP-MSU international multicenter randomized controlled trial.
View Article and Find Full Text PDFXOR-Derived ROS in Tie2-Lineage Cells Including Endothelial Cells Promotes Aortic Aneurysm Progression in Marfan Syndrome.
Arterioscler Thromb Vasc Biol
January 2025
Department of Cardiovascular Medicine, The University of Tokyo, Bunkyo-ku, Japan. (H. Yagi, H.A., Q.L., A.S.-K., M.U., H.K., R.M., A.S., S.O., H.T., Norifumi Takeda, I.K.).
Background: Marfan syndrome (MFS) is an inherited disorder caused by mutations in the gene encoding fibrillin-1, a matrix component of extracellular microfibrils. The main cause of morbidity and mortality in MFS is thoracic aortic aneurysm and dissection, but the underlying mechanisms remain undetermined.
Methods: To elucidate the role of endothelial XOR (xanthine oxidoreductase)-derived reactive oxygen species in aortic aneurysm progression, we inhibited in vivo function of XOR either by endothelial cell (EC)-specific disruption of the gene or by systemic administration of an XOR inhibitor febuxostat in MFS mice harboring the missense mutation p.
Accurate lamb origin identification and molecular differentiation analysis using rapid evaporative ionization mass spectrometry.
Anal Methods
January 2025
Chinese Academy of Inspection and Quarantine, Beijing 100176, China.
Rapid and accurate methods for tracing and identifying the origin of lamb are crucial for ensuring food authenticity and quality. This study developed a precise traceability method to determine the origin of lamb by integrating rapid evaporative ionization mass spectrometry (REIMS) with multivariate statistical analysis. Lamb samples from Xilin Gol, Ordos, and Hulun Buir ranches were identified by REIMS fingerprinting within 1 min.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!