- Asymmetric Hydroboration of Heteroaryl Ketones by Aluminum Catalysis
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A series of methyl aluminum complexes bearing chiral biphenol-type ligands were found to be highly active catalysts in the asymmetric reduction of heterocyclic ketones (S/C = 100-500, ee up to 99%). The protocol is suitable for a wide range of substrates and has a high tolerance to functional groups. The formed 2-heterocyclic-alcohols are valuable building blocks in drug discovery or can be used as ligands in asymmetric catalysis. Isolation and comprehensive characterization of the reaction intermediates support a catalysis cycle proposed by DFT calculations.
- Lebedev, Yury,Polishchuk, Iuliia,Maity, Bholanath,Dinis Veloso Guerreiro, Miguel,Cavallo, Luigi,Rueping, Magnus
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Read Online
- Straight from the bottle! Wine and juice dicarboxylic acids as templates for supramolecular cage self-assembly
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Two imine based supramolecular cages are able to self-assemble in the presence of a complex mixture like wine or fruit juices. Taking advantage of templating agents present in these mixtures the systems are able to form and to selectively encapsulate dicarboxylic systems present in the mixtures. This capability has been exploited to develop molecular systems able to report the enantiomeric excess and composition of (a)chiral dicarboxylic acids in fruit juices and wines using 1H-NMR. This journal is
- Begato, Federico,Penasa, Roberto,Licini, Giulia,Zonta, Cristiano
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supporting information
p. 10019 - 10022
(2021/10/07)
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- CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED BY TERTIARY HYDROXY GROUPS AS PI3K-GAMMA INHIBITORS
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This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-y which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
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Page/Page column 261-262
(2019/05/10)
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- Modulators of methyl modifying enzymes, compositions and uses thereof
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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Page/Page column 185; 186; 190
(2015/12/26)
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- ACETYLENIC MICROBIOCIDES
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Compounds of formula (I), wherein the other substituents HetAr, A', R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in claim 1, and their use in compositions and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
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Page/Page column 36
(2013/10/21)
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- CONDENSED TRICLYCLIC COMPOUNDS AS INHIBITORS OF HIV REPLICATION
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Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted -(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inbitor of HIV replication.
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- Antibacterial Compounds
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The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
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Paragraph 0525
(2013/10/07)
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- PHENICOL ANTIBACTERIALS
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The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
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Paragraph 0419
(2013/09/26)
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- NOVEL BENZOXAZINE OXAZOLIDINONE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
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Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following formula (I), preparation method
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Paragraph 0113
(2013/04/23)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein
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Paragraph 00385; 00396; 00397
(2013/06/05)
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- Novel substituted (pyridin-3-yl)phenyloxazolidinones: Antibacterial agents with reduced activity against monoamine oxidase A and increased solubility
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Oxazolidinones represent a new and promising class of antibacterial agents. Current research in this area is mainly concentrated on improving the safety profile and the antibacterial spectrum. Oxazolidinones bearing a (pyridin-3-yl)phenyl moiety (e.g., 3) generally show improved antibacterial activity compared to linezolid but suffer from potent monoamine oxidase A (MAO-A) inhibition and low solubility. We now disclose the finding that new analogues of 3 with acyclic substituents on the pyridyl moiety exhibit excellent activity against Gram-positive pathogens, including linezolid-resistant Streptococcus pneumoniae. Generally, more bulky substituents yielded significantly reduced MAO-A inhibition relative to the unsubstituted compound 3. The MAO-A SAR can be rationalized on the basis of docking studies using a MAO-A/MAO-B homology model. Solubility was enhanced with incorporation of polar groups. One optimized analogue, compound 13, showed low clearance in the rat and efficacy against S. pneumoniae in a mouse pneumonia model.
- Reck, Folkert,Zhou, Fei,Eyermann, Charles J.,Kern, Gunther,Carcanague, Dan,Ioannidis, Georgine,Illingworth, Ruth,Poon, Grace,Gravestock, Michael B.
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p. 4868 - 4881
(2008/03/12)
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- 3- {4- (PYRIDIN-3-YL) PHENYL} -5- (1H-1, 2, 3-TRIAZOL-1-YLMETHYL) -1, 3-OXAZOLIDIN-2-ONES AS ANTIBACTERIAL AGENTS
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Compounds of formula (I), as well as pharmaceutically-acceptable salts and pro-drugs thereof, are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
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