- VISIBLE-LIGHT MEDIATED ORGANOPHOTOREDOX CATALYTIC DEUTERATION OF AROMATIC AND ALIPHATIC ALDEHYDES
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Described are methods for preparing a deuterated aldehyde using with a photocatalyst and a hydrogen atom transfer agent in a H2O free solvent comprising D2O and an organic solvent under an inert gas. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions.
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Paragraph 0069-0070
(2021/06/22)
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- NOVEL AMINOPHOSPHINIC DERIVATIVES AS AMINOPEPTIDASE A INHIBITORS
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The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.
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Page/Page column 24
(2020/06/10)
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- AMINOPEPTIDASE A INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.
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Page/Page column 31
(2020/06/10)
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- Aminoquinazoline derivatives and their use in medicine
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The invention provides aminoquinazoline derivatives, or their stereoisomers, geometric isomers, tautomers, despinners, nitrogen oxides, hydrates, solvates, metabolites, metabolism precursors and pharmaceutically acceptable salts or prodrugs. The above compounds can be used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the above compounds and a use of the above compounds or their pharmaceutical composition in preparation of drugs for treating proliferative diseases.
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Paragraph 0624; 0631-0633
(2019/11/29)
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- DIPEPTIDE AND TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
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Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.
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Paragraph 00340; 00343
(2014/10/04)
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- Synthetic strategies for the synthesis and transformation of substituted pyrrolinones as advanced intermediates for rhazinilam analogues
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The biaryl core structure of rhazinilam with its fixed dihedral angle is a pivotal element for its unique in vitro cytotoxic activity. Most of the related natural products are oxidized versions of rhazinilam. Replacing the sensitive pyrrole ring by a pyrrolinone ring is the basis of our initial strategy towards rhazinilam analogues. With this goal, variants of the sequence crossed Mukaiyama aldol reaction followed by the Staudinger reaction were studied. Reacting a suitably substituted acetophenone with O-methyl O-trimethylsilyl ketene acetal gave pyrrolinones 8a and 8b in good to excellent yields. These intermediates could be transformed in four high-yielding steps into the pyrrolic precursors 7a-c containing all the atoms necessary for the construction of rings A, B, and C of rhazinilam. Our studies illustrate a lack of stability of these intermediates. Alternative synthetic approaches towards this central biaryl core structure are described.
- Kholod, Inga,Vallat, Olivier,Buciumas, Ana-Maria,Neels, Antonia,Neier, Reinhard
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supporting information
p. 7865 - 7877
(2015/03/04)
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- Highly enantioselective epoxidation of α,β-unsaturated ketones catalyzed by primary-secondary diamines
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The asymmetric epoxidation of α,β-unsaturated ketones has been achieved by using functional and readily accessible primary-secondary diamines as the catalysts, giving the useful alkyl epoxy products with good yields and high enantioselectivities (up to 99% ee). Copyright
- Lu, Yingpeng,Zheng, Changwu,Yang, Yingquan,Zhao, Gang,Zou, Gang
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supporting information; experimental part
p. 3129 - 3133
(2012/01/03)
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- Synthesis of enantiomerically pure α-amino-β-hydroxy- cyclobutanone derivatives and their transformations into polyfunctional three- and five-membered ring compounds
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Ketenes readily cycloadded to (R)-tert-butyldihydrooxazole 2a-d to yield enantiomerically pure bicyclic cyclobutanones. The cycloadditions proceeded with unusual regiochemistry giving predominantly or exclusively protected α-amino-β-hydroxycyclobutanone derivatives. The adducts could be converted into a variety of interesting enantiopure intermediates equipped with many functional groups: α-amino-β-hydroxy cyclopropane carboxylic acid derivatives, α-amino-β-hydroxy succinic acid derivatives, α-amino-β-hydroxy lactones and lactams derivatives.
- Ghosez, Léon,Yang, Gaoqiang,Cagnon, José Renato,Bideau, Franck Le,Marchand-Brynaert, Jacqueline
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p. 7591 - 7606
(2007/10/03)
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- From alkenylsilanes to ketones with air as the oxidant
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Air and water are required for a tandem intermolecular radical addition-oxidation sequence that converts alkenylsilanes into a variety of ketones. The reaction of 2-silyl1-alkenes with various carbon-centered radicals (see scheme) provides carbonyl compounds in good yields, This process represents a novel oxidative transformation of organosilicon compounds with molecular oxygen as the oxidant. R3Si = MePh2Si, Me2PhSi, R1 = Me, Ph, CO2Me, SiMe2Ph, R2 = CH2COR′ (R′ = OBn, NEt2, OnBu, Ph), C6F13.
- Kondo, Junichi,Shinokubo, Hiroshi,Oshima, Koichiro
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p. 825 - 827
(2007/10/03)
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- A sterically-encumbered, C2-symmetric chiral acetal for enhanced asymmetric induction in the Pauson-Khand reaction
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High levels of diastereoselection were achieved in the PKR, of 1,6- and 1,7-cyclopropylidenynes bearing a bulky propargylic C2-symmetric acetal.
- Krafft, Marie E.,Bonaga, Llorente V. R.,Felts, Andrew S.,Hirosawa, Chitaru,Kerrigan, Sean
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p. 6039 - 6042
(2007/10/03)
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- Probing the activities and mechanisms of leukotriene A4 hydrolase with synthetic inhibitors
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Leukotriene (LT) A4 hydrolase catalyzes the hydrolysis of leukotriene A4 to form leukotriene B4, a potent inflammatory mediator. Recently, the synthesis and evaluation of the highly effective competitive LTA4 hydrolase inhibitor 2 (K(i) = 1.6 nM) was described. In the present study, we describe the biological activity of 2 against LTB4 biosynthesis, as well as the design, synthesis, and evaluation of a new series of inhibitors intended to probe the active site of the enzyme. On the basis of these results and of previously reported site-directed mutagenesis and inhibition studies, the mechanisms of peptide and epoxide hydrolysis catalyzed by LTA4 hydrolase are discussed.
- Hogg, J. Heather,Ollmann, Ian R.,Wetterholm, Anders,Andberg, Martina Blomster,Haeggstroem, Jesper,Samuelsson, Bengt,Wong, Chi-Huey
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p. 1698 - 1713
(2007/10/03)
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- Influence of the ester group during the enantioselective methylation of α-aldehyde esters via their chiral oxazolidine derivatives
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Depending on the nature of the ester group, fair asymmetric induction (ee's up to 82%) can be attained in the title reaction.
- Agami, Claude,Couty, Franc ois
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p. 5659 - 5660
(2007/10/02)
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