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Synthesis of 1,4-diarylpyrrolotriazepine derivatives by two diverse strategies

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Abstract

1,4-Diaryl-5H-pyrrolo[2,1-d][1,2,5]triazepines were prepared by two different pathways. In the first case, the condensation reaction of the appropriate diketones with hydrazine monohydrate was applied for the construction of the seven-membered triazepine ring. In the second case, previously prepared intermediates, 1-aryl-3H-pyrrolo[2,1-d][1,2,5]triazepine-4(5H)-thiones were used as starting materials. The arylation of these thioamides were carried out with boronic acids in Liebeskind-Srogl palladium-catalysed cross-coupling reaction.

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Authors and Affiliations

  1. Egis Pharmaceuticals Plc., Directorate of Drug Substance Development, P. O. Box 100, Budapest, 1475, Hungary

    Tamás Földesi, András Dancsó, Gyula Simig, Balázs Volk & Mátyás Milen

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  1. Tamás Földesi
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  2. András Dancsó
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  3. Gyula Simig
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  4. Balázs Volk
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  5. Mátyás Milen
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Correspondence to Mátyás Milen.

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Földesi, T., Dancsó, A., Simig, G. et al. Synthesis of 1,4-diarylpyrrolotriazepine derivatives by two diverse strategies. Monatsh Chem 147, 1975–1983 (2016). https://doi.org/10.1007/s00706-016-1831-6

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  • DOI: https://doi.org/10.1007/s00706-016-1831-6

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