- Direct Synthesis of Pyrroles via Heterogeneous Catalytic Condensation of Anilines with Bioderived Furans
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Given the wide applications of pyrroles in agriculture, pharmaceuticals, and supramolecular and materials chemistry, a mild and eco-friendly route to produce functionalized pyrroles from bioderived feedstocks is highly desirable. Described herein is a mild and convenient synthesis of pyrroles via direct condensation of an equimolar amount of structurally diverse anilines with biobased furans catalyzed by a simple and efficient solid acid H form zeolite Y catalyst. The protocol tolerates a large variety of functional groups and offers a general and versatile method for scale-up synthesis of a variety of N-substituted pyrrole compounds. Most importantly, the bioactive pyrrole-derived drug pyrvinium, which has lately been confirmed as highly effective in curing colon cancer, can be obtained by this method.
- Tao, Lei,Wang, Zi-Jian,Yan, Tian-Hao,Liu, Yong-Mei,He, He-Yong,Cao, Yong
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p. 959 - 964
(2017/08/09)
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- Synthesis, radiolabeling and evaluation of novel amine guanidine derivatives as potential positron emission tomography tracers for the ion channel of the N-methyl-d-aspartate receptor
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The N-Methyl-d-Aspartate receptor (NMDAR) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. The aim of this study was to develop a positron emission tomography (PET) ligand to assess the bio-availa
- Klein, Pieter J.,Chomet, Marion,Metaxas, Athanasios,Christiaans, Johannes A.M.,Kooijman, Esther,Schuit, Robert C.,Lammertsma, Adriaan A.,Van Berckel, Bart N.M.,Windhorst, Albert D.
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p. 143 - 160
(2016/05/09)
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- Greener Paal-Knorr Pyrrole Synthesis by Mechanical Activation
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A straightforward and solventless synthesis of pyrroles was developed by using mechanochemical activation and a biosourced organic acid as the catalyst. Relative to traditional Paal-Knorr methodologies, various N-substituted pyrroles were obtained in very short reaction times. By reaction with unreactive diketones, desymmetrized aliphatic and aromatic compounds were also synthesized.
- Akelis, Liudvikas,Rousseau, Jolanta,Juskenas, Robertas,Dodonova, Jelena,Rousseau, Cyril,Menuel, Stphane,Prevost, Dominique,Tumkeviius, Sigitas,Monflier, Eric,Hapiot, Frdric
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