- Copper-Catalyzed Asymmetric Diyne Cyclization via [1,2]-Stevens-Type Rearrangement for the Synthesis of Chiral Chromeno[3,4-c]pyrroles
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Here, we report a copper-catalyzed asymmetric cascade cyclization/[1,2]-Stevens-type rearrangement via a non-diazo approach, leading to the practical and atom-economic assembly of various valuable chiral chromeno[3,4-c]pyrroles bearing a quaternary carbon
- Hong, Feng-Lin,Hong, Pan,Lu, Xin,Shi, Chong-Yang,Ye, Long-Wu,Zhai, Tong-Yi,Zhu, Xin-Qi
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- Preparation and Reactions of Mono- and Bis-Pivaloyloxyzinc Acetylides
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Mono-pivaloyloxyzinc acetylide and bis-pivaloyloxyzinc acetylide were selectively prepared from ethynylmagnesium bromide in quantitative yields. These zinc reagents readily underwent Negishi cross-couplings with (hetero)aryl iodides or bromides as well as subsequent Sonogashira cross-couplings. 1,3-Dipolar cycloadditions of these zinc acetylides with benzylic azides produced zincated and bis-zincated triazoles which were trapped with several electrophiles. An opposite regioselectivity compared to the Cu-catalyzed click-reactions was observed.
- Tüllmann, Carl Phillip,Chen, Yi-Hung,Schuster, Robin J.,Knochel, Paul
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supporting information
p. 4601 - 4605
(2018/08/09)
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- Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists
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Herein, we report studies leading to the discovery of the neoseptins and a comprehensive examination of the structure-activity relationships (SARs) of this new class of small-molecule mouse Toll-like receptor 4 (mTLR4) agonists. The compounds in this class, which emerged from screening an α-helix mimetic library, stimulate the immune response, act by a well-defined mechanism (mouse TLR4 agonist), are easy to produce and structurally manipulate, exhibit exquisite SARs, are nontoxic, and elicit improved and qualitatively different responses compared to lipopolysaccharide, even though they share the same receptor.
- Morin, Matthew D.,Wang, Ying,Jones, Brian T.,Su, Lijing,Surakattula, Murali M. R. P.,Berger, Michael,Huang, Hua,Beutler, Elliot K.,Zhang, Hong,Beutler, Bruce,Boger, Dale L.
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supporting information
p. 4812 - 4830
(2016/06/13)
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- NEOSEPTINS: SMALL MOLECULE ADJUVANTS
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A MD-2:TLR4 complex agonist compound is disclosed whose structure corresponds to Formula (I), as defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.
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Page/Page column 42-44
(2014/09/03)
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- A New Preparation of Benzofurans Utilizing Trimethylsilyldiazomethane
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o-Triisopropylsiloxyaryl ketones and aldehydes smoothly reacted with the lithium salt of trimethylsilyldiazomethane to give o-triisopropylsiloxyphenylacetylenes which were easily converted to benzofurans by treatment with tetra-n-butylammonium fluoride. 3-Benzofuranmethanols were also obtained when the reaction was conducted in the presence of carbonyl compounds.
- Ito, Yasuko,Aoyama, Toyohiko,Shioiri, Takayuki
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p. 1163 - 1164
(2007/10/03)
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