- Regiochemistry of the microwave-assisted reaction between aromatic amines and α-bromoketones to yield substituted 1H-indoles
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The scope and regioselectivity of the Bischler (or Bischler-Moehlau) reaction between aromatic amines and α-bromoketones has been studied by computational and experimental techniques. It has been found that in many cases the reaction yields are improved under microwave irradiation and working in the absence of solvent. When di- and trisubstituted amines are used as substrates the regioselectivity of the reaction is different to that obtained with the corresponding primary anilines. The reaction between benzene-1,2-diamine and α-bromoacetophenones under the same conditions yields 2-substituted quinoxalines instead of indoles. Finally, when pyridin-2-amines and pyrimidine-2-amines are allowed to react with the corresponding α-bromoacetophenones, the corresponding imidazo[1,2-a]pyridines and imidazo[1,2-a]pyrimidines are obtained, respectively. The Royal Society of Chemistry.
- Vara, Yosu,Aldaba, Eneko,Arrieta, Ana,Pizarro, Jose L.,Arriortua, Maria I.,Cossio, Fernando P.
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experimental part
p. 1763 - 1772
(2008/10/09)
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- INDOLE-CONTAINING COMPOUNDS WITH ANTI-TUBULIN AND VASCULAR TARGETING ACTIVITY
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Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin assembly. Such compounds as well as related derivatives are excellent clinical candidates for the
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- Methods of treating neuropeptide Y-associated conditions
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This invention describes methods of treating conditions associated with an excess of neuropeptide Y which comprises administering an analog of an obesity protein. This invention further describes methods of treating conditions associated with an excess of neuropeptide Y which coomprises administering an analog of an obesity protein in combination with a neuropeptide Y antagonist. This invention demonstrates that the obesity protein acts by reducing the production of neuropeptide Y by the hypothalamus.
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- Methods for treating resistant tumors
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The present invention provides methods for reversing multidrug resistance in a resistant neoplasm by treating a mammal in need of said treatment with a substituted indole, benzofuran, benzothiophene, naphthalene, or dihydronaphthalene. This invention also provides methods for treating neoplasms in a mammal which comprises administering to a mammal in need of this treatment a substituted indole, benzofuran, benzothiophene, naphthalene, or dihydronaphthalene in combination with an oncolytic agent.
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- Methods of treating nueropeptide Y-associated conditions
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This invention describes methods of treating conditions associated with an excess of neuropeptide Y which comprises administering an obesity protein. This invention also describes methods of treating conditions associated with an excess of neuropeptide Y which comprises administering an obesity protein in combination with a neuropeptide Y antagonist. This invention demonstrates that the obesity protein acts by reducing the production of neuropeptide Y by the hypothalamus.
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- Methods of treating neuropeptide Y-associated conditions
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This invention describes methods of treating conditions associated with an excess of neuropeptide Y which coomprises administering an analog of an obesity protein. This invention further describes methods of treating conditions associated with an excess of neuropeptide Y which coomprises administering an analog of an obesity protein in combination with a neuropeptide Y antagonist. This invention demonstrates that the obesity protein acts by reducing the production of neuropeptide Y by the hypothalamus.
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- HETEROCYCLIC NEUROPEPTIDE Y RECEPTOR ANTAGONISTS
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This invention provides methods for treating or preventing a condition associated with an excess of neuropeptide Y which methods comprise administration of one or more substituted benzofurans, benzothiophenes or indoles.
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- Methods of treating neuropeptide Y-associated conditions
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This invention describes methods of treating conditions associated with an excess of neuropeptide Y which comprises administering a naturally occurring obesity protein. Another embodiment of this invention describes methods of treating conditions associated with an excess of neuropeptide Y which comprises administering a naturally occurring obesity protein in combination with a neuropeptide Y antagonist. This invention demonstrates that the obesity protein acts by reducing the production of neuropeptide Y by the hypothalamus.
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- 2-(hydroxy-phenyl)-indoles and process for their production
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Pharmaceutical compositions are provided containing a 2-(hydroxyphenyl)-indole or a 2-(C2 -C6 -alkanoxyloxyphenyl) indole and a pharmaceutically acceptable carrier.
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- 2-Phenyl-indole derivatives
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The present invention relates to new stabilizers of polymers and co-polymers of vinyl chloride corresponding to the general formula: STR1 wherein R1, R2, R3, R4, R5 and R6, which are the sa
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