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Synfacts 2011(12): 1267-1267
DOI: 10.1055/s-0031-1289315
DOI: 10.1055/s-0031-1289315
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag
Stuttgart ˙ New York
Synthesis of PF-03463275
M. A. Berliner*, S. P. A. Dubant, T. Makowski, K. Ng, B. Sitter, C. Wager, Y. Zhang
Pfizer Global Research and Development, Groton, USA; Pfizer Global Research and Development, Sandwich, UK
Further Information
Publication History
Publication Date:
18 November 2011 (online)
Significance
PF-03463275 is a glycine transporter type 1 (GlyT1) inhibitor that has potential for the treatment of schizophrenia. The synthesis depicted features the first kilogram-scale application of iridium-catalyzed hydrogen borrowing to achieve the operational equivalent of reductive amination in the union of C and D to give E. The only byproduct of the reaction is water.