- METHOD FOR CONVERTING HYDROXYL GROUP OF ALCOHOL
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The present invention relates to: a method for converting a hydroxyl group of an alcohol; and a catalyst which makes the method possible. A method for converting a hydroxyl group of an alcohol according to the present invention is characterized by producing a compound represented by CH(R1)(R2)Nu (wherein R1, R2 and Nu are as defined below) by reacting an alcohol represented by CH(R1)(R2)OH (wherein each of R1 and R2 represents a hydrogen atom, an optionally substituted alkyl group, or the like) and a compound having an active proton, which is represented by H-Nu (wherein Nu represents a group represented by —CHX1-EWG1 or —NR3R4; X1 represents a hydrogen atom or the like; EWG1 represents an electron-withdrawing group; and each of R3 and R4 represents a hydrogen atom, an optionally substituted alkyl group, or the like), with each other in the presence of a complex of a group 7-11 metal of the periodic table and at least one solid base that is selected from the group consisting of layered double hydroxides, composite oxides and calcium hydroxide.
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Paragraph 0373; 0376-0377
(2021/02/19)
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- NOVEL COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE
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A compound represented by the following formula (1):
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- PYRROLOPYRAZINE KINASE INHIBITORS
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The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
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Page/Page column 226; 227
(2013/03/28)
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- Metal complexes of tetra(6-tert-butyl-2,3-quinolino)porphyrazine: I. Synthesis
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Complexes of tetra(6-tert-butyl-2,3-quinolino)porphyrazine with Cu, Co, Zn, and Ni soluble in hydrophobic liquids were synthesized for the first time by template tetramerization of derivatives of 6-tert-butylquinoline-2,3- dicarboxylic acid formed from the corresponding acid in the course of carbamide synthesis in presence of the bivalent metal ions.
- Efimova,Korzhenevskii,Koifman
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scheme or table
p. 1614 - 1621
(2009/06/28)
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- HETEROCYCLIC NON-PEPTIDE GNRH ANTAGONISTS
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A compound of formula (I): wherein either B is absent and A and Z are the same or different and are each hydrogen, halogen, alkyl, hydroxy, alkoxy,-CN,-C(Rc)2OH,-N(Rd)C(=X)Rc,-C(=X)N(Rc)(Rd),-S(O)m-Rc,-N(Rc)(Rd)S(O)2,-S(O)2N(R c)(Rd),-N(Re)2, aryl optionally substituted with Ra or-O-aryl optionally substituted with Ra; or B is present and is-(CH2)n-,-C(Rb)2-or-O-, or B taken together with A or Z can be-C=C(Rb)-,-C(Rb)=C-,-CH2-CH(R b)-or-CH(Rb)-CH2-; D is-O-or-S(O) m,-; E is a bond or is-(CH2)n-,-N(R d)-,-(CH2)nN(Rd)-or-N(R d)(CH2)n-; F is-C(=X)-; G is-(CH2 )n-,-N(Rd)-,-(CH2)nN(R d)-or-N(Rd)(CH2)n; J is a bond,-O-,-N(RC)C(=X)-,-C(=X)N(Rc)-,-S(O)m,-,-N(Rc)S(O)m-,-S(O)nN(Rc)-,-N(Re)-or-N(Rg)(Rh); K is a bond, alkylene, cycloalkylene, cycloalkenylene, arylene, heterocycloalkylene, heterocycloalkylene or heteroarylene; and L is hydrogen or a terminal group; has therapeutic utility.
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Page/Page column 35; 49-50
(2008/06/13)
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- Oxidative dearomatization of phenols and anilines via λ3 - and λ5-iodane-mediated phenylation and oxygenation
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Treatment of 2-methylphenols with chloro(diphenyl)-λ3- iodane led to their regioselective dearomatizing 2-phenylation into cyclohexa-2,4-dienone derivatives via a proposed ligand coupling reaction. In the same vein of investigation, treatment of 2-methylanilines with the λ5-iodane 2-iodoxybenzoic acid IBX reagent led to their regioselective dearomatization into previously undescribed ortho-quinol imines.
- Quideau, Stephane,Pouysegu, Laurent,Ozanne, Aurelie,Gagnepain, Julien
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p. 201 - 216
(2007/10/03)
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- Compounds useful as anti-inflammatory agents
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Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
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- 5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: Potent nonpeptidic inhibitors of HIV protease
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On the basis of previous SAR findings and molecular modeling studies, a series of compounds were synthesized which possessed various sulfonyl moieties substituted at the 4-position of the C-3 phenyl ring substituent of the dihydropyran-2-one ring system. The sulfonyl substituents were added in an attempt to fill the additional S3' pocket and thereby produce increasingly potent inhibitors of the target enzyme. Racemic and enantiomerically resolved varieties of selected compounds were synthesized. All analogues in the study displayed decent binding affinity to HIV protease, and several compounds were shown to possess very good antiviral efficacy and safety margins. X-ray crystallographic structures confirmed that the sulfonamide and sulfonate moieties were filling the S3' pocket of the enzyme. However, the additional substituent did not provide improved enzymatic inhibitory or antiviral activity as compared to the resolved unsubstituted aniline. The addition of the sulfonyl moiety substitution does not appear to provide favorable pharamacokinectic parameters. Selected inhibitors were tested for antiviral activity in clinical isolates and exhibited similar antiviral activity against all of the HIV-1 strains tested as they did against the wild-type HIV-1. In addition, the inhibitors exhibited good antiviral efficacies against HIV-1 strains that displayed resistance to the currently marketed protease inhibitors.
- Boyer, Frederick E.,Vara Prasad,Domagala, John M.,Ellsworth, Edmund L.,Gajda, Christopher,Hagen, Susan E.,Markoski, Larry J.,Tait, Bradley D.,Lunney, Elizabeth A.,Palovsky, Alexander,Ferguson, Donna,Graham, Neil,Holler, Tod,Hupe, Donald,Nouhan, Carolyn,Tummino, Peter J.,Urumov,Zeikus, Eric,Zeikus, Greg,Gracheck, Stephen J.,Sanders, James M.,VanderRoest, Steven,Brodfuehrer, Joanne,Iyer, Krishna,Sinz, Michael,Gulnik, Sergei V.,Erickson, John W.
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p. 843 - 858
(2007/10/03)
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- Nonpeptidic HIV protease inhibitors: 6-Alkyl-5, 6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl, 5-methylphenyl thio) moiety: Antiviral activities and pharmacokinetic properties
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Dihydropyran-2-ones possessing amino and carboxamide functionalities on 3-SPh (2-tert-butyl, 5-methyl) ring were synthesized and evaluated for their antiviral activities. Both the enantiomers of inhibitor 15 were synthesized. The in vitro resistance profi
- Vara Prasad,Boyer, Fred E.,Domagala, John M.,Ellsworth, Edmund L.,Gajda, Christopher,Hagen, Susan E.,Markoski, Larry J.,Tait, Bradley D.,Lunney, Elizabeth A.,Tummino, Peter J.,Ferguson, Donna,Holler, Tod,Hupe, Donald,Nouhan, Carolyn,Gracheck, Stephen J.,VanderRoest, Steven,Saunders, James,Iyer, Krishna,Sinz, Michael,Brodfuehrer, Joanne
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p. 1481 - 1486
(2007/10/03)
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- Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety
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Dihydropyran-2-ones possessing a sulfamate moiety at the 4-position of the thiophenyl ring were designed to reach S3' pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2-t- butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indices will be described.
- Vara Prasad,Markoski, Larry J.,Boyer, Fred E.,Domagala, John M.,Ellsworth, Edmund L.,Gajda, Christopher,Hagen, Susan E.,Tait, Bradley D.,Lunney, Elizabeth A.,Tummino, Peter J.,Ferguson, Donna,Holler, Tod,Hupe, Donald,Nouhan, Carolyn,Gracheck, Stephen J.,VanderRoest, Steven,Saunders, James,Iyer,Sinz
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p. 2217 - 2222
(2007/10/03)
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