- A novel access to 4-trifluoromethyl-1,3-thiazole derivatives via an intermediate thiocarbonyl ylide
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A Lewis acid catalyzed reaction of trifluoroacetyldiazomethane (CF3COCHN2) with thiourea occurs in boiling THF solution in the presence of BF3·OEt2 yielding 2-amino-4-trifluoromethyl-1,3-thiazole in a fair yield
- Obijalska, Emilia,B?aszczyk, Magdalena,Kowalski, Marcin K.,Mlostoń, Grzegorz,Heimgartner, Heinz
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- NOVEL COMPOUNDS WITH A 3A-AZABICYCLO [4.1.0] HEPTANE CORE ACTING ON OREXIN RECEPTORS
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This invention relates to azabicyclo[4.1.0]hept-4-yl derivatives and their use as pharmaceuticals.
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Page/Page column 38-39
(2012/07/14)
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- Thiazolides as novel antiviral agents. 2. Inhibition of hepatitis c virus replication
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We report the activities of a number of thiazolides [2-hydroxyaroyl-N- (thiazol-2-yl)amides] against hepatitis C virus (HCV) genotypes IA and IB, using replicon assays. The structure-activity relationships (SARs) of thiazolides against HCV are less predic
- Stachulski, Andrew V.,Pidathala, Chandrakala,Row, Eleanor C.,Sharma, Raman,Berry, Neil G.,Lawrenson, Alexandre S.,Moores, Shelley L.,Iqbal, Mazhar,Bentley, Joanne,Allman, Sarah A.,Edwards, Geoffrey,Helm, Alison,Hellier, Jennifer,Korba, Brent E.,Semple, J. Edward,Rossignol, Jean-Francois
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supporting information; experimental part
p. 8670 - 8680
(2012/02/16)
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- CARBACEPHEM BETA-LACTAM ANTIBIOTICS
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Carbacephem β-lactam antibiotics having chemical structures (I) and (II) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R6 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 65; 88
(2010/11/05)
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- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem -lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar1, Ar2, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 92
(2010/04/06)
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- FUSED PYRIMIDINEONE COMPOUNDS AS TRPV3 MODULATORS
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The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are pro
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Page/Page column 20
(2009/12/05)
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- THIAZOLE PYRAZOLOPYRIMIDINES AS CRF1 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological dise
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Page/Page column 43
(2008/06/13)
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- ARYL SULFONES AND USES RELATED THERETO
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Aryl sulfone compounds of formula (I) and (II) are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders.
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Page/Page column 92
(2010/02/14)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Positive allosteric modulators of the nicotinic acetylcholine receptor
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The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which α7 nAChR is known to be involved.
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- α- or β-Trifluoromethyl epoxysulfones: new C3 reagents for heterocyclisation
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The syntheses of α- and β-trifluoromethyl epoxysulfones 1 and 2 are described.Compound 1 reacts with nucleophiles and bis-nucleophiles to furnish trifluoromethyl ketones and trifluoromethyl heterocycles in good yield, while its isomer 2 leads to the opposite thiazole regioisomers with thioamides. - Keywords: Trifluoromethyl epoxysulfones; Heterocyclisation; Regioisomers; NMR spectroscopy; IR spectroscopy
- Laduron, Frederic,Janousek, Zdenek,Viehe, Heinz, G.
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- Synthesis of Trifluoromethylthiazoles and Their Application to Azo Dyes
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3-Bromo-1,1,1-trifluoropropan-2-one (2) reacted with thiourea and N-monosubstituted thiourea to give the corresponding 4-trifluoromethylthiazoles, respectively.In the reactions with N,N'-diphenylthiourea and thioamides, the considerably stable intermediat
- Tanaka, Kiyoshi,Nomura, Kazuto,Oda, Hitoshi,Yoshida, Shouhei,Mitsuhashi, Keiryo
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p. 907 - 911
(2007/10/02)
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- Syntheses of Trifluoromethyl Heterocycles
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Mono and bicyclic heterocycles bearing trifluoromethyl substituent have been synthesized and characterized by spectral studies. 4(5)-Trifluoromethylimidazole (3) is prepared from the reaction of 3,3-dibromo-1,1,1-trifluoroacetone (2) with formaldehyde and ammonia.N-Methylation of 3 by phase transfer reaction gives 1-methyl-4-trifluoromethylimidazole (4). 2-Amino-4-trifluoromethylimidazole (5) is similarly obtained from 3-bromo-1,1,1-trifluoroacetone (1) and thiourea.The reaction of 1 with 2-aminopyridine and 2-aminothiazole gives 2-trifluoromethylimidazopyridine (7) and 6-trifluoromethylimidazothiazole (9) respectively.
- Moazzam, Muhammad,Parrick, J.
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p. 1051 - 1053
(2007/10/02)
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- An Infrared Study of Rotational Isomerism in Thiazole-2-carboxylates
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A series of alkyl thiazole-2-carboxylates containing a range of substituents at the 4- and 5-positions has been prepared.Solutions of these esters (mostly new compounds) show well resolved doublets in the i.r.C=O region which arise from rotational isomers.The higher wavenumber components are assigned to the more polar carbonyl O,S-anti-s-trans-rotamers and the lower wavenumber components to the carbonyl O,S-syn-s-trans-forms.Small, but systematic, differences between the methyl esters are noted.
- Kaye, Perry T.,Meakins, G. Denis,Willbe, Charles,Williams, Peter R.
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p. 2335 - 2339
(2007/10/02)
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