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New stereoselective syntheses of cis- and trans-2-methyl-4-arylpiperidines |
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| Authors: | Alain Merschaert Laurent DelhayeJean-Paul Kestemont Willy BrionePieter Delbeke Vincent MancusoFreddy Napora Khalid DikerDaniel Giraud Michel Vanmarsenille |
| Institution: | Chemical Process Research and Development, Lilly Research Laboratories, Lilly Development Centre S.A., rue Granbonpré 11, 1348 Mont-Saint-Guibert, Belgium |
| Abstract: | A stereoselective approach has been developed for the synthesis of cis- and trans-2-methyl-4-arylpiperidines from a common intermediate. The Ni-catalyzed hydrogenolysis of N-Boc-2-methyl-4-aryl-4-piperidinols, obtained by addition of organometallic reagents on N-Boc-2-methyl-4-piperidone, afforded the trans derivatives with up to 95% selectivity whereas the corresponding cis isomers were obtained in the presence of palladium catalysts. |
| Keywords: | hydrogenolysis nickel palladium piperidines |
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