- Total Synthesis and Bioactivity Studies of Fungal Metabolite (-)-TAN-2483B
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The first total synthesis of (-)-TAN-2483B, a fungal metabolite possessing a densely functionalized furo[3,4-b]pyran-5-one framework, is achieved in 14 steps from d-mannose. Generation of the 2,6-trans-pyran is by cyclopropane ring expansion followed by α-selective alkynylation. Julia-Kocienski olefination introduces the E-propenyl side chain. Alkyne functionalization and carbonylation stereoselectively establish the bicyclic core of (-)-TAN-2483B. Inhibition of kinases Btk and Bmx, bacterial priority pathogens, and cytokine production in splenocytes indicates promising therapeutic potential.
- McCone, Jordan A. J.,Somarathne, Kalpani K.,Orme, Christopher L.,Hewitt, Russell J.,Grant, Elysha-Rose,Hall, Kelsi R.,Ackerley, David F.,La Flamme, Anne C.,Harvey, Joanne E.
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- Cobalt Single-Atom-Intercalated Molybdenum Disulfide for Sulfide Oxidation with Exceptional Chemoselectivity
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The identification of chemoselective oxidation process en route to fine chemicals and specialty chemicals is a long-standing pursuit in chemical synthesis. A vertically structured, cobalt single atom-intercalated molybdenum disulfide catalyst (Co1-in-MoS2) is developed for the chemoselective transformation of sulfides to sulfone derivatives. The single-atom encapsulation alters the electron structure of catalyst owing to confinement effect and strong metal–substrate interaction, thus enhancing adsorption of sulfides and chemoselective oxidation at the edge sites of MoS2 to achieve excellent yields of up to 99% for 34 examples. The synthetic scopes can be extended to sulfide-bearing alkenes, alkynes, aldehydes, ketones, boronic esters, and amines derivatives as a toolbox for the synthesis of high-value, multifunctional sulfones and late-stage functionalization of pharmaceuticals, e.g., Tamiflu. The synthetic utility of cobalt single atom-intercalated MoS2, together with its reusability, scalability, and simplified purification process, renders it promising for industrial productions.
- Chen, Zhongxin,Liu, Cuibo,Liu, Jia,Li, Jing,Xi, Shibo,Chi, Xiao,Xu, Haisen,Park, In-Hyeok,Peng, Xinwen,Li, Xing,Yu, Wei,Liu, Xiaowang,Zhong, Linxin,Leng, Kai,Huang, Wei,Koh, Ming Joo,Loh, Kian Ping
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- SULFAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES
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The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
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Page/Page column 18
(2017/09/15)
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- METHOD FOR PRODUCING ALKENE STEREOSELECTIVELY
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PROBLEM TO BE SOLVED: To provide a method for producing alkene efficiently and stereoselectively, and tetrazole that is a reaction intermediate useful for the production method and represented by formula (2). SOLUTION: The present invention provides a met
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- Phosphabarrelenes as ligands in rhodium-catalyzed hydroformylation of internal alkenes essentially free of alkene isomerization
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Despite significant research efforts in the past, one of the remaining problems to be solved in industrially important hydroformylation is the chemoselective low-pressure hydroformylation of internal alkenes. We report here on a new class of phosphabarrelene/rhodium catalysts 2 that display very high activity towards hydroformylation of internal alkenes with an unusually low tendency towards alkene isomerization. Preparation of new phosphabarrelene ligands, studies of their coordination properties, as well as results obtained in the rhodium-catalyzed hydroformylation of cyclic and acyclic internal alkenes are reported.
- Fuchs, Evelyn,Keller, Manfred,Breit, Bernhard
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p. 6930 - 6939
(2007/10/03)
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- THIA-EPOTHILONE DERIVATIVES FOR THE TREATMENT OF CANCER
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The present invention relates to new Macrocycles of formula (I) and their use for the treatment of cancer.
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- A synthesis of herboxidiene
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The natural herbicide herboxidiene was constructed from two key fragments using a modified Julia olefination based on the benzothiazolyl sulfone activator. Key steps in the synthesis of the C1-C10 oxane fragment were (a) a modified Julia olefination using
- Blakemore, Paul R.,Kocienski, Philip J.,Morley, Andrew,Muir, Kenneth
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p. 955 - 968
(2007/10/03)
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