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Efficient Synthesis of Phosphono‐ and Phosphinoxidomethylated N‐Heterocycles under Solvent‐Free Microwave Conditions
Authors:Ibolya Prauda  István Greiner  Krisztina Ludányi
Institution:1. Department of Organic Chemical Technology , Budapest University of Technology and Economics , Budapest, Hungary;2. Gedeon Richter Ltd. , Budapest, Hungary;3. Hungarian Academy of Sciences, Chemical Research Center , Budapest, Hungary;4. Semmelweis University Faculty of Pharmacy, Department of Pharmaceutics , Budapest, Hungary
Abstract:Simple N‐heterocycles were converted to N‐phosphono‐ and phosphinoxidomethyl derivatives by a solvent‐free microwave‐assisted condensation of the heterocycle, paraformaldehyde, and diethylphosphite or diphenylphosphine oxide in a convenient and, in most cases, efficient way. In contrast to an earlier report, imidazole proved to be unreactive in this type of phospha‐Mannich reaction.
Keywords:α‐aminomethylphosphine oxides  α‐aminomethylphosphonates  green chemistry  N‐heterocycles  microwave synthesis  solvent‐free method
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