- Catalytic Asymmetric Intermolecular Cyclopropanation of a Ketone Carbene Precursor by a Ruthenium(II)-Pheox Complex
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The diazo derivative of acetonyl acetate is a useful basic skeleton for the synthesis of cyclopropyl ketones. The intermolecular cyclopropanations of diazo acetoxy acetone with olefins are accomplished by using a novel p-nitro-Ru(II)-diphenyl-Pheox catalyst to give the corresponding optically active cyclopropane derivatives in good yields (up to 95%) with excellent diastereoselectivities (up to 99:1) and enantioselectivities (up to 98% ee). (Figure presented.).
- Chi, Le Thi Loan,Suharto, Agus,Da, Ho Linh,Chanthamath, Soda,Shibatomi, Kazutaka,Iwasa, Seiji
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p. 951 - 955
(2019/01/25)
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- SUBSTITUTED DIHYDROPYRAZOLO PYRAZINE CARBOXAMIDE DERIVATIVES
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The invention relates to substituted dihydropyrazolo pyrazine carboxamide derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and diabetes, and also urogenital and ophthalmic disorders.
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Page/Page column 83
(2020/01/10)
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- Enantioselective Synthesis of N-Benzylic Heterocycles: A Nickel and Photoredox Dual Catalysis Approach
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Reported herein is a dual nickel- and photoredox-catalyzed modular approach for the preparation of enantioenriched N-benzylic heterocycles. α-Heterocyclic carboxylic acids, easily obtainable from common commercial material, are reported as suitable substrates for a decarboxylative strategy in conjunction with a chiral pyridine-oxazoline (PyOx) ligand, providing quick access to enantioenriched drug-like products. The presence of a directing group on the heterocyclic moiety is shown to be beneficial, affording improved stereoselectivity in a number of cases.
- Pezzetta, Cristofer,Bonifazi, Davide,Davidson, Robert W. M.
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supporting information
p. 8957 - 8961
(2019/11/11)
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- ERK INHIBITORS
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Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.
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- N -heteropolycyclic compounds from the formal intramolecular (4 + 1)-cycloaddition of chromium aminocarbenes
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Chromium aminocarbenes tethered to dienes of all three electronic natures undergo an efficient intramolecular (4 + 1)-cycloaddition to give N-heteropolycyclic compounds. Ligands on chromium had a profound effect on the course of the reaction.
- Dery, Martin,Lefebvre, Louis-Philippe D.,Aissa, Kevin,Spino, Claude
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supporting information
p. 5456 - 5459
(2013/11/19)
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- BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF
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The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic u
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Page/Page column 69-70
(2012/02/06)
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- HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
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The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
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Page/Page column 33
(2010/04/25)
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- Substituted pteridines for the treatment of inflammatory diseases
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The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as
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Page/Page column 8
(2010/11/08)
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- Ruthenium-catalyzed asymmetric epoxidation of olefins using H 2O2, part I: Synthesis of new chiral N,N,N,-tridentate pybox and pyboxazine ligands and their ruthenium complexes
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The synthesis of chiral tridentate N,N,N-pyridine-2.6-bisoxazolines 3 (pyhox ligands) and N,N,N-pyridine-2.6-bisoxazines 4 (pyboxazine ligands) is described in detail. These novel ligands constitute a useful tool-box for the application in asymmetric catalysis. Compounds 3 and 4 are conveniently prepared by cyclization of enantiomerically pure α- or β-amino al cohols with dimethyl pyridine-2,6-dicarboximidate. The corresponding ruthenium complexes are efficient asymmetric epoxidation catalysts and have been prepared in good yield and fully char acterized by spectroscopic means. Four of these ruthenium complexes have been characterized by X-ray crystallography. For the first time the molecular structure of a pyboxazine complex (2,6-bis-[(4S)-4-phenyl-5,6- dihydro-4H-[1,3]oxazinyl]pyridine)(pyridine-2,6-dicarboxylate)ruthenium (S)-2aa, is presented.
- Tse, Man Kin,Bhor, Santosh,Klawonn, Markus,Anilkumar, Gopinathan,Jiao, Haijun,Doebler, Christian,Spannenberg, Anke,Magerlein, Wolfgang,Hugl, Herbert,Beller, Matthias
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p. 1855 - 1874
(2008/02/02)
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- Stereoselective nucleophilic addition with a new chiral template and its application to the synthesis of optically active α-arylglycine derivatives
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Mannich-type reaction of phenols with iminolactone 4, readily prepared from commercially available phenylglycine, proceeded with high stereoselectivity to give α-arylglycine derivatives. The reaction was also applicable to other electron-rich aromatic compounds, arylboronic acids and other nucleophiles. Additionally, several Lewis acid-promoted addition reactions with iminolactone 4 were accomplished efficiently. These adducts could be converted readily to the corresponding optically active α-amino acid derivatives.
- Tohma, Shigemitsu,Rikimaru, Kentaro,Endo, Atsushi,Shimamoto, Keiko,Kan, Toshiyuki,Fukuyama, Tohru
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p. 909 - 917
(2007/10/03)
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- C2-Symmetric Bis(oxazolinato)lanthanide Catalysts for Enantioselective Intramolecular Hydroamination/Cyclization
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C2-symmetric bis(oxazolinato)lanthanide complexes of the type [(4R,5S)-Ph2Box]La[N(TMS)2]2, [(4S,5R)-Ar 2Box]La[N(TMS)2]2, and [(4S)-Ph-5,5-Me 2Box]La[N(TMS)2/su
- Hong, Sukwon,Tian, Shun,Metz, Matthew V.,Marks, Tobin J.
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p. 14768 - 14783
(2007/10/03)
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- Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
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- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
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- HIGHLY ENANTIOSELECTIVE CATALYTIC DIELS-ALDER ADDITION PROMOTED BY A CHIRAL BIS(OXAZOLINE)-MAGNESIUM COMPLEX
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The new chiral bis(oxazoline) ligand 8 has been synthesized from (S)-phenylglycine and has been shown to form effective catalysts for enantioselective Diels-Alder addition in combination with ferric iodide, magnesium iodide or magnesium tetraphenylborate.Catalytic activation of the dienophile, 3-acryloyl-1,3-oxazolidine-2-one (4), in the magnesium system is proposed to involve tetrahedrally coordinated magnesium in a dispositive complex (10).
- Corey, E. J.,Ishihara, Kazuaki
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p. 6807 - 6810
(2007/10/02)
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