Synthesis, Table of Contents Synthesis 2017; 49(09): 2057-2062DOI: 10.1055/s-0036-1588133 paper © Georg Thieme Verlag Stuttgart · New YorkA Borrowing Hydrogen Approach to the Synthesis of RS-67,333 Authors Author Affiliations Elodie Carbonnel VFP Therapies, R & D Laboratory, IRCOF, Rue Tesnière, 76131 Mont Saint Aignan, France Email: vgembus@vfp-therapies.com Florent Alix VFP Therapies, R & D Laboratory, IRCOF, Rue Tesnière, 76131 Mont Saint Aignan, France Email: vgembus@vfp-therapies.com Vincent Gembus* VFP Therapies, R & D Laboratory, IRCOF, Rue Tesnière, 76131 Mont Saint Aignan, France Email: vgembus@vfp-therapies.com Recommend Article Abstract Buy Article(opens in new window) All articles of this category(opens in new window) Abstract A new strategy using the borrowing hydrogen methodology to access the 5-HT4R agonist RS-67,333 is presented. Especially, this selective and highly potent ligand of 5-HT4 receptor was obtained quickly and efficiently by catalytic alkylation of a ketone with various alcohols in the presence of a catalytic amount of (Cp*IrCl2)2. Key words Key wordsiridium - catalysis - hydrogen transfer - alcohols - heterocycles Full Text References References 1a Meltzer CC, Smith G, DeKosky ST, Pollock BG, Mathis CA, Moore RY, Kupfer DJ, Reynolds CF. Neuropsychopharmacology 1998; 18: 407 1b Reynolds GP, Mason SL, Meldrum A, De Keczer S, Parnes H, Eglen RM, Wong EH. F. Br. J. Pharmacol. 1995; 114: 993 1c Bockaert J, Ansanay H, Waeber C, Sebben M, Fagni L, Dumuis A. CNS Drugs 1994; 1: 6 Selected references: 2a Darcet F, Gardier AM, David DJ, Guilloux J.-P. Neurosci. Lett. 2016; 616: 197 2b Claeysen S, Bockaert J, Giannoni P. ACS Chem. Neurosci. 2015; 6: 940 2c Quiedeville A, Boulouard M, Hamidouche K, Da Silva Costa-Aze V, Nee G, Rochais C, Dallemagne P, Fabis F, Freret T, Bouet V. Behav. 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