An efficient synthesis of 2,5-disubstituted-3-cyanoindoles is described. This approach utilizes a highly selective iodination together with the modified Made lung reaction to generate an intermediate which can be readily transformed to more fully elaborated 2,5-disubstituted-3-cyanoindole templates that were previously difficult to access. Detailed examples and utility of this approach are presented herein. (C) 2011 Elsevier Ltd. All rights reserved.
An efficient synthesis of 2,5-disubstituted-3-cyanoindoles is described. This approach utilizes a highly selective iodination together with the modified Made lung reaction to generate an intermediate which can be readily transformed to more fully elaborated 2,5-disubstituted-3-cyanoindole templates that were previously difficult to access. Detailed examples and utility of this approach are presented herein. (C) 2011 Elsevier Ltd. All rights reserved.
The present invention is related to new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Open Vessel and Cooling while Heating Microwave-Assisted Synthesis of Pyridinyl <i>N</i>-Aryl Hydrazones
作者:Giuseppe La Regina、Valerio Gatti、Francesco Piscitelli、Romano Silvestri
DOI:10.1021/co100015b
日期:2011.1.10
We reported the first example of open vessel and cooling while heating microwave-assisted synthesis of pyridinyl N-aryl hydrazones. Compounds were prepared in excellent isolated yields (88-98%) in only 5 min, by reacting 4- and 2,4-(di) substituted phenylhydrazines, bearing both electron-donating (4-CH3, 4-OCH3) and -withdrawing (4-Cl, 4-Br, 4CF(3), 4-NO2, 2,4-Cl-2) groups with 2-, 3-, and 4-acetylpyridine. The method was successfully extended to other carbonyl compounds.