A new synthetic route to compounds of the AFDX-type with affinity to muscarinic M2-receptor |
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Authors: | Ulrike Holzgrabe Eberhard Heller |
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Affiliation: | Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, D-97074 Würzburg, Germany |
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Abstract: | [3-(1,3-Dioxo-1,3-dihydroisoindol-2-yl)-propyl]dimethyl-{6-[(1-{2-[(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepine-11-carbonyl)amino]ethyl}piperidin-2-yl-methyl)-propylamino]hexyl}ammonium bromide a hybride containing a fragment of the antagonist of muscarinic receptor AFDX-384 and a W84 moiety known as allosteric modulator of antagonist binding, was synthesized in a divergent synthesis starting from pipecolic acid, phthalic anhydride and 3-amino-2-chloropyridine. This new microwave assisted route is very convenient and allows to modify the piperidine ring, the benzodiazepine system, the phthalimide moiety and the chains connecting the ring systems. Yields and reproducibility were satisfying. |
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Keywords: | AFDX-384 W84 microwave assisted reaction AFDX-384-W84 hybride |
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