- Facile preparation and reactivity of polymer-supported N-(2-lodyl-phenyl)- acylamide, an Efficient Oxidizing System
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(Chemical Equation Presented) A simple three-step preparation of polymer-supported N-(2-iodyl-phenyl)-acylamide (NIPA resin) starting from 2-iodoaniline is described. The resin was obtained with good loading levels (0.7-0.8 mmol g-1) and has been successfully used for efficient oxidation of a diverse collection of alcohols. Thus, treating alcohols with 1.0 equiv of the resin in 1,2-dichloroethane under reflux for 30-60 min allowed rapid and in most cases complete conversion to the corresponding carbonyl compound.
- Ladziata, Uladzimir,Willging, Jeff,Zhdankin, Viktor V.
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- Selective metallation of thiophene and thiazole rings with magnesium amide base
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The chemoselective magnesiation of thiophene and thiazole derivatives were reported using magnesium chloride. Organomagnesium compounds were used at relatively higher temperatures. The results showed that hydrogen-magnesium exchange reaction of thiophene derivatives with iPr2NMgCl proceeded selectively.
- Shilai, Manabu,Kondo, Yoshinori,Sakamoto, Takao
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- Conjugated compounds based on vinylthiazole units
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Conjugated compounds based on vinylthiazole units show a strong polarization along the π chain, when NR2 groups as electron donors are attached in the terminal position. The effect can be even more enhanced by a CHO group as electron acceptor in the opposite terminal position. This property makes such oligomers (n = 1, 2, . . .) interesting for applications in linear and nonlinear optics.
- Meier, Herbert,Nicklas, Frank,Petermann, Ralf
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- Synthesis of nonlinear optical chromophores containing electron-excessive and -deficient heterocyclic bridges. The auxiliary donor-acceptor effects
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Push-pull substituted nonlinear optical chromophores with thiazole and thiophene rings and interposed ethylene units as π-conjugated bridges were synthesized. The effects of the nature and location of the heterocycles on the energy of the charge transfer transition for the chromophores are discussed.
- Shu, Ching-Fong,Wang, Yuh-Kai
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- INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
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Paragraph 00539
(2018/07/05)
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- HIV INTEGRASE INHIBITORS
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The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
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- Synthesis of 2,5-di(hydroxyalkyl)-1,3-thiazoles
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A general approach towards synthesis of 2(5)-hydroxyalkyl-substituted 1,3-thiazole derivatives has been proposed. The method includes lithiation of 1,3-thiazole ring followed by reacting the formed thiazole lithium derivatives with electrophiles.
- Sinenko,Slivchuk,Bal'On, Ya. G.,Brovarets
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p. 1855 - 1861
(2015/10/12)
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- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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Paragraph 0174 - 0175
(2014/05/24)
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- SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
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Page/Page column 386; 387
(2014/09/29)
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- SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
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Paragraph 0304; 0305
(2014/09/30)
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- A general method for the enantioselective synthesis of α-chiral heterocycles
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The enantioselective formation of stereocenters proximal to unprotected heterocycles has been accomplished. Thus, vinyl boronic acids are added to heterocycle-appended enones via a modified-BINOL catalyst. Catalyst design was key to enable a general reaction. High yields and useful er's are observed for a host of common heteroaryls.
- Le, Phong Q.,Nguyen, Thien S.,May, Jeremy A.
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supporting information
p. 6104 - 6107
(2013/02/23)
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- Development of new recyclable reagents and catalytic systems based on hypervalent iodine compounds
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Recent advances in the development of polymer-supported iodine(V) oxidants, recyclable monomeric hypervalent iodine(III) reagents and catalytic systems based on hypervalent iodine compounds are discussed. These efficient and environmentally friendly reagents and catalysts are particularly useful for oxidative transformations of alcohols to carbonyl compounds and for oxidations at the benzylic position.
- Yusubov, Mekhman S.,Zhdankin, Viktor V.
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experimental part
p. 185 - 191
(2011/03/19)
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- BICYCLONONENE DERIVATIVES AS RENIN INHIBITORS
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The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
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Page/Page column 36
(2008/06/13)
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- BICYCLIC FIVE-MEMBERED HETEROARYL DERIVATIVES AND THEIR USE AS RENIN INHIBITORS
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The invention relates to novel five-membered heteroaryl derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions comprising one or more of those compounds and especially their use as inhibitors of renin.
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Page/Page column 22
(2010/11/23)
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- Isoquinoline compound melanocortin receptor ligands and methods of using same
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The invention relates to melanocortin receptor ligands and methods of using the ligands to alter or regulate the activity of a melanocortin receptor. The invention further relates to tetrahydroisoquinoline aromatic amines that function as melanocortin receptor ligands and as agents for controlling cytokine-regulated physiologic processes and pathologies, and combinatorial libraries thereof.
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- Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
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Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
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- METHANOANTHRACENEYL METHYL PIPERIDINYL COMPOUNDS
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Compounds of formula I or I', STR1 wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;R 1 is selected from(A) (1-6C)alkyl; (B) phenyl and naphthyl or substituted versions thereof; (C) phenyl (1-3C)alkyl and naphthyl (1-3C) alkyl;(D) five-and six-membered heteroaryl rings;(E) heteroaryl (1-3C) alkyl and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I or I' and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I or I', or a pharmaceutically acceptable salt thereof are claimed. The invention also relates to novel processes for producing enantiomeric methanoanthracenyl sulfoxides.
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- Tetrahydronaphthyl and thiazole, oxazole or imidazole substituted ethene derivatives having retinoid-like activity, reduced skin toxicity and reduced teratogenecity
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Compounds of the formula STR1 as herein defined, have retinoid-like activity and are substantially non-teratogenic and non-irritating to the skin.
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- Total Synthesis of (+)-Galactostatin. An Illustration of the Utility of the Thiazole-Aldehyde Synthesis
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The natural aza sugar (+)-galactostatin (+)-1 has been prepared from D-serine by sequential installation of chiral 1C and 2C units employing thiazole-based reagents.Thus, the D-serine-derived methyl ester 3 was transformed by 2-thiazolyllithium (4) into t
- Dondoni, Alessandro,Perrone, Daniela
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p. 4749 - 4754
(2007/10/02)
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- 1,2,3-TRIAZOLOTHIAZOLES; SYNTHESIS AND PROPERTIES
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The synthesis of 1,2,3-triazolothiazole (15) and its 3-methyl- (16) and 3-phenyl- (17) derivatives is reported, together with their spectra, quaternisation, and ring opening reactions.
- Jones, Gurnos,Ollivierre, Hermione,Fuller, L. S.,Young, J. H.
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p. 2851 - 2860
(2007/10/02)
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- A New Convenient Preparation of 2-, 4-, and 5-Thiazolecarboxaldehydes and Their Conversion into the Corresponding Carbonitrile N-Oxides: Synthesis of 3-Thiazolylisoxazoles and 3-Thiazolylisoxazolines
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The title aldehydes are prepared in high yields by quenching 2-lithiothiazole, 4-lithio-, and 5-lithio-2-trimethylsilylthiazole with N-formylmorpholine followed by protodesilylation in the latter two cases.The aldehydes are transformed through their oxime
- Dondoni, Alessandro,Fantin, Giancarlo,Fogagnolo, Marco,Medici, Alessandro,Pedrini, Paola
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p. 998 - 1001
(2007/10/02)
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- N-aminomethyl-2-amino(and 2-amino-methyl)-2-(2-quinolyl)-thioacetamides
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The compounds are N-aminomethyl-2-amino(and 2-aminomethyl)-2-heterocyclic-thioacetamides which are inhibitors of gastric acid secretion.
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- 2-Alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides
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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.
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