- Acid-catalysed Aromatisation of Benzene cis-1,2-dihydrodiols: a Carbocation Transition State poorly stabilised by Resonance
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Acid-catalysed dehydration of 3-substituted benzene cis-1,2-dihydrodiols exhibits a Hammett plot with ρ=-8.2, consistent with reaction via a benzenonium ion-like intermediate; however, correlation of +M resonance substituents such as Me and MeO by ?p rather than ?+ constants indicates a marked imbalance between resonance and inductive stabilisation of the transition state.
- Boyd, Derek R.,Blacker, John,Byrne, Briege,Dalton, Howard,Hand, Mark V.,et al.
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- Aerobic oxynitration of alkynes with tBuONO and TEMPO
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An efficient method for stereoselective nitroaminoxylation of alkyne has been reported. The reaction enjoys a broad substrate scope, good functional group tolerance, and high yields. Synthetically useful α-nitroketones can be accessed through these products in a single step.
- Dutta, Uttam,Maity, Soham,Kancherla, Rajesh,Maiti, Debabrata
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- BTK Inhibitors and uses thereof
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The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
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Paragraph 1480; 1486-1488
(2020/05/02)
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- Tetrafluoropyridyl (TFP): a general phenol protecting group readily cleaved under mild conditions
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Phenols are extremely valuable building blocks in the areas of pharmaceuticals, natural products, materials and catalysts. In order to carry out modifications on phenols, the phenolic oxygen is routinely protected to prevent unwanted side reactions. Presently many of the protecting groups available can require harsh conditions, specialist equipment, expensive or air/moisture-sensitive reagents to install and remove. Here we introduce the use of the tetrafluoropyridyl (TFP) group as a general protecting group for phenols. TFP can be installed in one step with no sensitivity to water or air, and it is stable under a range of commonly employed reaction conditions including acid and base. The TFP protecting group is readily cleaved under mild conditions with quantitative conversion to the parent phenol, observed in many cases in less than 1 hour.
- Brittain, William D. G.,Cobb, Steven L.
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supporting information
p. 2110 - 2115
(2019/02/27)
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- HETEROCYCLIC DERIVATIVES MODULATING ACTIVITY OF CERTAIN PROTEIN KINASES
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The present invention relates to novel heterocyclic derivatives having general formula (I) and their therapeutic use for diseases such as cancer, inflammation, pain, autoimmune diseases or neurodegenerative diseases like Alzheimer's or Parkinson's disease that can be treated by modulation of certain protein kinases. Compounds of formula (I) can be used for treatment of patients who do not respond to kinase inhibition therapy that comprises currently available medications.
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- Acetylenes from Aldehydes. Preparation of Ethynylphenols and Phenylacetylenes by Flash Vacuum Pyrolysis of Isoxazolones
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The flash vacuum pyrolysis method of synthesis of acetylenes from aldehydes via isoxazolones is a convenient method for the preparation of a variety of derivatives, including kinetically unstable, sensitive compounds such as the ethynylphenols.
- Wentrup, Curt,Wiedenstritt, Maria,Winter, Hans-Wilhelm
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p. 1233 - 1236
(2015/08/18)
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- INSECTICIDAL CARBAMATES EXHIBITING SPECIES-SELECTIVE INHIBITION OF ACETYLCHOLINESTERASE (AChE)
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The present invention includes insecticidal carbamates that are useful, for example, for the control of insects, such as mosquitoes, which can be used in applications where exposure to and/or contact with humans is likely. The insecticides of the present invention include phenyl N-methyl carbamates and compositions comprising them that exhibit species-selective inhibition of acetylcholinesterase (AChE) and are preferably toxic to mosquitoes but not humans. Of particular interest are compounds of Formula (I) and Formula (II): Compounds of Formula (I) and Formula (II) are especially suitable for insecticide treated nets and indoor residual spraying for mosquito control.
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Page/Page column 7
(2009/04/24)
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- Convenient syntheses of m- and p-ethynylphenols
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m-lodophenol (4a) was found to couple with 2-methylbut-3-yn-2-ol (5) in the presence of PdCl2-CuI-Ph3P-in triethylamine to afford 3-(3-hydroxy-3-methylbut-1-ynyl)phenol(6a), which was conveniently converted into m-ethynylphenol (7a). Under the same conditions, p-iodophenol did not couple with 5. However, p-iodo-1-[(tetrahydro-2H-pyran-2-yl)oxy]benzene (4b) did react with 5 to afford 1-[(tetrahydro-2H-pyran-2-yl)oxy]-4-[2-hydroxy-2-methyl- 4-but-3-ynyl]benzene (6b), which was similarly converted into 1-[(tetrahydro-2H-pyran-2-yl)oxy]-4-ethynylbenzene (7b) with loss of acetone. Removal of the tetrahydropyranyl protecting group from 7b furnished p-ethynylphenol (8).
- Lai, Guo-Qiao,Liu, Shi-Ling,Xu, Jin-Feng,Shen, Yong-Jia
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p. 203 - 204
(2007/10/03)
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- Enzymatic and Chemical Syntheses of cis-Dihydrodiol Derivatives of Monocyclic Arenes
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Metabolism of bromobenzene and iodobenzene by growing cultures of Pseudomonas putida UV4 gave the corresponding cis-dihydrodiol products 1 and 2 in high yields; subsequent direct chemical substitution of the halogen atoms in these metabolites provided a new range of enantiomerically pure cis-dihydrodiols of known absolute configuration.
- Boyd, Derek R.,Hand, Mark V.,Sharma, Narain D.,Chima, Jagdeep,Dalton, Howard,Sheldrake, Gary N.
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p. 1630 - 1632
(2007/10/02)
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- Ethynyl-substituted aromatic ortho diamines and method of synthesis
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As new compositions of matter, ethynyl-substituted aromatic ortho-diamines. The compounds are useful as endcapping agents for thermally stable heterocyclic oligomeric compositions.
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