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Functionalization of Piperidine Derivatives for the Site Selective and Stereoselective Synthesis of Positional Analogs of Methylphenidate

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Liu, Wenbin ; Babl, Tobias ; Röther, Alexander ; Reiser, Oliver ;
Date of publication of this fulltext: 22 Jan 2021 09:24

This publication is part of the DEAL contract with Wiley.


Rhodium-catalyzed C-H insertions and cyclopropanations of donor/acceptor carbenes have been used for the synthesis of positional analogues of methylphenidate. The site selectivity is controlled by the catalyst and the amine protecting group. C-H functionalization of N-Boc-piperidine using Rh-2(R-TCPTAD)(4), or N-brosyl-piperidine using Rh-2(R-TPPTTL)(4) generated 2-substitited analogues. In ...


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