- Synthesis of 2-(2-Oxo-2-phenylethyl)cyclopentanone by Rhodium-Catalyzed Tandem Alkynyl Cyclobutanols Hydroacylation and Semipinacol Rearrangement
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A rhodium-catalyzed tandem reaction of alkynyl cyclobutanols with salicylaldehydes has been developed. The reaction offers a new and atom-economical approach for the selective preparation of multisubstituted 2-(2-oxo-2-phenylethyl)cyclopentanone in high y
- Guo, Rui,Mo, Xueling,Zhang, Guozhu
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- SUBSTITUTED IMIDAZOLECARBOXYLATE DERIVATIVES AND THE USE THEREOF
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A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and/or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and/or preparation of a drug with sedative, hypnotic and/or anesthetic effects and controlling the state of epilepsy.
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Paragraph 0847-0849
(2020/12/08)
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- Structure-based design of tricyclic NF-κB inducing kinase (NIK) inhibitors that have high selectivity over phosphoinositide-3-kinase (PI3K)
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We report here structure-guided optimization of a novel series of NF-κB inducing kinase (NIK) inhibitors. Starting from a modestly potent, low molecular weight lead, activity was improved by designing a type 11/2 binding mode that accessed a back pocket past the methionine-471 gatekeeper. Divergent binding modes in NIK and PI3K were exploited to dampen PI3K inhibition while maintaining NIK inhibition within these series. Potent compounds were discovered that selectively inhibit the nuclear translocation of NF-κB2 (p52/REL-B) but not canonical NF-κB1 (REL-A/p50).
- Castanedo, Georgette M.,Blaquiere, Nicole,Beresini, Maureen,Bravo, Brandon,Brightbill, Hans,Chen, Jacob,Cui, Hai-Feng,Eigenbrot, Charles,Everett, Christine,Feng, Jianwen,Godemann, Robert,Gogol, Emily,Hymowitz, Sarah,Johnson, Adam,Kayagaki, Nobuhiko,Kohli, Pawan Bir,Knüppel, Kathleen,Kraemer, Joachim,Krüger, Susan,Loke, Pui,McEwan, Paul,Montalbetti, Christian,Roberts, David A.,Smith, Myron,Steinbacher, Stefan,Sujatha-Bhaskar, Swathi,Takahashi, Ryan,Wang, Xiaolu,Wu, Lawren C.,Zhang, Yamin,Staben, Steven T.
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supporting information
p. 627 - 640
(2017/02/05)
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- ANTIBACTERIAL AGENTS
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Antibacterial compounds of formula (I) are provided, as well as stereoisomers and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
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Page/Page column 60
(2013/12/03)
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- Catalytic enantioselective intermolecular desymmetrization of 3-substituted oxetanes
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Wring it out: The title reaction proceeds in the presence of chiral Bronsted acid catalysts. This efficient ring-opening process features low catalyst loading, mild reaction conditions, broad functional group compatibility, high enantioselectivity, and the capability to generate chiral quaternary centers. The highly functionalized desymmetrization products are versatile chiral building blocks in organic synthesis. Copyright
- Wang, Zhaobin,Chen, Zhilong,Sun, Jianwei
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supporting information
p. 6685 - 6688
(2013/07/26)
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