- Hydroaminomethylation with novel Rhodium-Carbene complexes: An efficient catalytic approach to pharmaceuticals
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Starting from [{Rh(cod)Cl}2] and 1,3-dimesitylimidazole-2- ylidenes the novel [RhCl(cod)(carbene)] complexes 1-5 have been synthesized, characterized, and tested in the hydroaminomethylation of aromatic olefins. The influence of different ligands and reaction parameters on the catalytic activity was investigated in detail applying 1,1-diphenylethylene and piperidine as a model system. The scope and limitations of the novel catalysts is shown in the preparation of 16 biologically active 1-amino-3,3-diarylpropenes. In general, high chemo- and regioselectivity as well as good yields of the desired products were achieved.
- Ahmed, Moballigh,Buch, Cathleen,Routaboul, Lucie,Jackstell, Ralf,Klein, Holger,Spannenberg, Anke,Beller, Matthias
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p. 1594 - 1601
(2008/02/04)
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- Preparation of pharmaceuticals by hydroformylation. Part III. The synthesis of N-(4-Pyridyl)-3,3-diphenyl-1-aminopropane (Phenpyramine, Milverine)
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N-(4-Pyridyl)-3,3-diphenyl-1-aminopropane (1) (Phenpyramine, Milverine), an important amino-pyridine derivative endowed with Muscarinic antagonist activity, is prepared starting from 1,1-diphenylethene using the hydroformylation as key the step in the reaction scheme: the obtained aldehyde was transformed in the desired compound 1 by a three steps reaction sequence; the overall yield was up to 42.8%.
- Marchetti,Sechi,Botteghi,Paganelli
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