- Selenium-catalyzed intramolecular atom- And redox-economical transformation ofo-nitrotoluenes into anthranilic acids
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Anthranilic acids (AAs) are significant basic chemicals used in pharmaceuticals, agrochemicals, dyes, fragrances,etc. Superfluous steps are always involved in obtaining AAs. Herein, we demonstrate a straightforward strategy to transform abundanto-nitrotoluenes into biologically and pharmaceutically significant AAs without any extra reductants, oxidants and protecting groups. Various sensitive groups, such as halogens, sulfide, aldehyde, pyridines, quinolines,etc., can be tolerated in this transformation. A hundred-gram-scale operation is realized efficiently with almost quantitative selenium recycling. Further mechanistic studies and DFT calculations disclosed the proposed atom-exchange processes and the key roles of the selenium species.
- Jiang, Xuefeng,Li, Yiming,Lin, Zhenyang,Wang, Yuhong,Yang, Tilong
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supporting information
p. 2986 - 2991
(2021/05/05)
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- METHODS AND COMPOUNDS FOR THE TREATMENT OF GENETIC DISEASE
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The present disclosure relates to compounds and methods for modulating the expression of dmpk, and treating diseases and conditions in which dmpk plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a nucleotide repeat sequence CAG or CTG; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence CAG or CTG; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.
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Paragraph 00616; 00706; 00707; 00708
(2021/08/13)
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- BICYCLIC HETEROCYCLE COMPOUNDS METHODS OF USE THEREOF FOR THE TREATMENT OF HERPES VIRUSES
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The present invention relates to novel Bicyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, X, Y, Z, R1 R5, R6, and R7 are as defined herein. The present invention also relates to compositions comprising
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Page/Page column 37
(2021/06/26)
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- Spiro-substituted pyrimido-cyclic compound, and preparation method and medical application thereof
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The invention discloses a spiro-substituted pyrimido-cyclic compound with selective inhibition effect on KRAS gene mutation and a pharmaceutically acceptable salt, a stereoisomer, a solvent compound or a prodrug thereof; the spiro-substituted pyrimido-cyclic compound is represented by a formula (I), and the definition of each group or symbol in the formula is shown in the specification in detail.In addition, the invention also discloses a pharmaceutical composition containing the compound and an application of the compound in preparation of cancer drugs.
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Paragraph 0218-0219; 0221
(2020/12/31)
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- SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS
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The present invention provides novel substituted imidazo[4,5-c]quinoline derivatives of formula (1), which may be therapeutically useful, more particularly as Bromodomain inhibitors; (1) in which Cyi, Cy2, R1, R2/sub
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