- Synthesis of N-alkyl-N′-aryl or Alkenylpiperazines: A Copper-Catalyzed C–N Cross-Coupling in the Presence of Aryl and Alkenyl Triflates and DABCO
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Unsymmetrical piperazines are key constituents of many pharmaceuticals. Given that the selective introduction of an aryl and alkyl motif onto the piperazine is not always straightforward, direct arylation and alkenylation of 1,4-diaza-bicyclo[2.2.2]octane would obviate the inefficiencies associated with the preparation of these target molecules. We have utilized alkyl halides, aryl or alkenyl triflates, and 1,4-diaza-bicyclo[2.2.2]octane for the synthesis of N-alkyl-N′-aryl or alkenylpiperazines. The optimum conditions are developed using CuCl, t-BuOLi in NMP. Alkenyl triflates requires N,N′-dimethylethylenediamine and higher temperature to afford the desired cross-coupled product. Substrates bearing electron-deficient and electron-rich groups were successfully coupled under the optimum reaction conditions.
- Ghazanfarpour-Darjani, Majid,Barat-Seftejani, Forugh,Khalaj, Mehdi,Mousavi-Safavi, Seyed Mahmoud
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- ODependent efficacy of novel piperidine- And piperazine-based chalcones against the human parasite giardia intestinalis
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Giardia intestinalis is the most frequent protozoan agent of intestinal diseases worldwide. Though commonly regarded as an anaerobic pathogen, it preferentially colonizes the fairly oxygen-rich mucosa of the proximal small intestine. Therefore, when testi
- Bahadur, Vijay,Mastronicola, Daniela,Tiwari, Hemandra K.,Kumar, Yogesh,Falabella, Micol,Pucillo, Leopoldo P.,Sarti, Paolo,Giuffre, Alessandro,Singh, Brajendra K.
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p. 543 - 549
(2014/01/17)
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- PHENYL-THIAZOLYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
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This invention relates to phenyl thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
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Page/Page column 34
(2012/12/13)
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- PIPERIDINE/PIPERAZINE DERIVATIVES
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The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -NRx -C(=O)-; -Z-C(=O)-; -Z-NRx -C(=O)-; -S(=O)p-; C(=S)-; -NRx -C(=S)-; -Z-C(=S)-; -Z-NRx -C(=S)-; -O-C(=O)-; -C(=O)-C(=O)-; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms,wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo- dioxinyl, 1,3-benzodioxolyl,2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
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Page/Page column 78-79
(2009/01/24)
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- A NEW CLASS OF HISTONE DEACETYLASE INHIBITORS
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New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH-NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or
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Page/Page column 79-80
(2008/06/13)
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- SELECTED CGRP ANTAGONISTS, METHOD FOR PRODUCTION AND USE THEREOF AS MEDICAMENT
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The invention relates to CGRP antagonists of general formula (I), in which A, U, V, W, X and R1 to R 3 are as defined in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures, salts, hydrates of the salts, in particular the physiologically-acceptable salts thereof with inorganic or organic acids, medicaments containing said compounds and the use and methods for production thereof.
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Page/Page column 120
(2008/06/13)
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- Solid-phase synthesis on functionalised fluoropolymer resins. Part 1: Nafion resin sulfonamide-immobilised carboxylic acid derivatives and aryl vinyl sulfones
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The preparation and properties of Nafion resin sulfonamide systems derived from methyl glycinate and from 3-hydroxyethylaniline are described. Nafion derivatisation reactions were slow and maximum achievable functionalisations were 50% of the ion exchange
- Akhtar, Mahmoud,Kroll, Friedrich E.K.,Gani, David
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p. 4487 - 4491
(2007/10/03)
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