- Functionalized 4-aminoquinolines by rearrangement of pyrazole N-heterocyclic carbenes
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(Figure Presented) Thermal decarboxylation of 1-phenyl pyrazolium-3- carboxylates from the mesomeric betaine class of substances leads to pyrazole-N-heterocyclic carbenes, which immediately rearrange to multiply substituted 4-aminoquinolines (see scheme). These species are of interest for the synthesis of heterocycles and pharmacologically active compounds.
- Schmidt, Andreas,Muenster, Niels,Dreger, Andrij
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supporting information; experimental part
p. 2790 - 2793
(2010/07/04)
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- Rearrangements of N-heterocyclic carbenes of pyrazole to 4-aminoquinolines and benzoquinolines
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1-Phenyl-substituted pyrazolium salts, formed by quaternization of pyrazoles with benzyl halides or long-chain alkyl halides, deprotonate to pyrazol-3-ylidenes that undergo a sequence of ring-opening, ring-closure, and tautomerization to new substituted 4
- Dreger, Andrij,Cisneros Camuna, Rafael,Munster, Niels,Andras Rokob, Tibor,Papai, Imre,Schmidt, Andreas
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experimental part
p. 4296 - 4305
(2010/10/19)
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- AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
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