Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Chiral Pool Synthesis of N-Cbz-cis-(3R,4R)-3-methylamino-4-methylpiperidine from L-Malic acid

  • Hao, Bao-Yu (Department of Chemical and Biological Engineering, Zhejiang University) ;
  • Liu, Jin-Qiang (Department of Chemical and Biological Engineering, Zhejiang University) ;
  • Zhang, Wei-Han (Hutchison MediPharma Limited) ;
  • Chen, Xin-Zhi (Department of Chemical and Biological Engineering, Zhejiang University)
  • Received : 2013.01.14
  • Accepted : 2013.02.07
  • Published : 2013.05.20
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Abstract

A new synthetic route to N-Cbz-cis-(3R,4R)-3-methylamino-4-methylpiperidine, key intermediate for CP-690,550, was disclosed with L-malic acid as the chiral pool starting material. The title compound was obtained in 16 steps with a total yield of 26% and more than 98% ee.

Keywords

References

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