- 2-Fluoro-5-nitrophenyldiazonium: A Novel Sanger-Type Reagent for the Versatile Functionalization of Alcohols
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As a novel Sanger-type reagent, 2-fluoro-5-nitrophenyldiazonium tetrafluoroborate enabled the versatile functionalization of primary and secondary aliphatic alcohols. Based on a mild nucleophilic aromatic substitution of the fluorine atom under unprecedented, base-free conditions, the diazonium unit on the aromatic core of the resulting aryl-alkyl ether could be employed for such diverse transformations as radical C?H activation and cyclization, as well as palladium catalyzed cross-coupling reactions.
- Fischer, Oliver,Heinrich, Markus R.
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supporting information
p. 5417 - 5421
(2021/03/01)
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- PHENAZINES AS INHIBITORS OF DISCOIDIN DOMAIN RECEPTORS 2 (DDR2)
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The invention concerns a compound of Formula (I) or a pharmaceutically acceptable salt or derivative thereof, wherein R1 and R2 are independently H or a group -O(CHR5)nR6, where n is an integer value from 1 to 3, R5 is independently H or CH3 for each integer value of n, R6 is H, an optionally substituted saturated heterocyclic ring or NR7R8, where R7 and R8 are independently H or (C1-C3)alkyl, R4 is H or CH3, R3 is a group selected from the group consisting of an optionally substituted aryl, (C3-C6)alkyl, benzyl, an optionally substituted saturated (C3-C6)cycloalkyl and an optionally substituted unsaturated heterocyclic ring for use as a medicament. The compounds as medicament are used in the treatment (DDR2)-mediated diseases and disorders such as a cancer, acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, atherosclerosis, various fibrotic disorders, fibrosis or kidney injury.
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Page/Page column 23
(2020/10/21)
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- Synthesis and antimicrobial studies of new antibacterial azo-compounds active against staphylococcus aureus and listeria monocytogenes
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Some novel (phenyl-diazenyl)phenols (4a–m) were designed and synthesized to be evaluated for their antibacterial activity. Starting from an active previously-synthesized azobenzene chosen as lead compound, we introduced some modifications and optimization of the structure, in order to improve solubility and drug conveyance. Structures of all newly-synthesized compounds were confirmed by 1H nuclear magnetic resonance (NMR), mass spectrometry, and UV-Vis spectroscopy. Antibacterial activity of the new compounds was tested with the dilution method against the bacteria strains Listeria monocytogenes, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa PAO1. All the compounds were selectively active against Gram-positive bacteria. In particular, compounds 4d, 4h, and 4i showed the highest activity against S. aureus and Listeria monocytogenes, reaching remarkable MIC100 values of 4 μg/mL and 8 μg/mL. The relationship between antimicrobial activity and compound structure has suggested that the presence of hydroxyl groups seems to be essential for antimicrobial activity of phenolic compounds.
- Piotto, Stefano,Concilio, Simona,Sessa, Lucia,Diana, Rosita,Torrens, Gabriel,Juan, Carlos,Caruso, Ugo,Iannelli, Pio
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 89; 90
(2013/10/22)
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- 4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES
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The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.
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Page/Page column 43
(2010/08/08)
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- An efficient intermolecular BINAM-copper(I) catalyzed Ullmann-type coupling of aryl iodides/bromides with aliphatic alcohols
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A wide range of alkyl aryl ethers are synthesized from the corresponding aryl iodides and aliphatic alcohols through Ullmann-type intermolecular coupling reactions in the presence of a catalytic amount of easily available BINAM-CuI complex. Less reactive aryl bromides have also been shown to react with aliphatic alcohols under identical reaction conditions to give good yields of the alkyl aryl ethers without increasing the reaction temperature and time.
- Naidu, Ajay B.,Sekar
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p. 3147 - 3151
(2008/09/20)
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- AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
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- Tetrahydronaphtalene derivatives, their preparation and pharmaceutical compositions containing them
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The invention provides compounds which are tetrahydronaphthalene derivatives of the formula (I) STR1 wherein R1 represents a halogen atom, a cyano group, a nitro group, an unbranched (C1 -C6) alkoxy group, a (C1
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- Studies on antihyperlipidemic agents. III. Synthesis and biological activities of 2-chloro-3-arylpropionic acids containing a quarternary carbon atom
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A series of 2-chloro-3-(4-alkoxyphenyl)propionic acids containing a quarternary carbon atom in the alkoxy moiety was prepared and the hypolipidemic and hypoglycemic activities were evaluated. Of the 18 compounds synthesized, ethyl 2-chloro-3-[4-(2-methyl-2-phenylpropyloxy)phenyl]propionate was the best with respect to biological activity and toxicity. Its functional derivatives and optically resolved enantiomers were also prepared. Structure-activity relationships are discussed briefly.
- Kawamatsu,Asakawa,Saraie,Mizuno,Imamiya,Nishikawa,Hamuro
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p. 751 - 758
(2007/10/02)
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