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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 5
BKCSDE 34(5)
May 20, 2013 

Chiral Pool Synthesis of N-Cbz-cis-(3R,4R)-3-methylamino-4-methylpiperidine from L-Malic acid
Bao-Yu Hao, Jin-Qiang Liu*, Wei-Han Zhang, Xin-Zhi Chen
N-Cbz-cis-(3R,4R)-3-methylamino-4-methylpiperidine, CP-690,550, L-Malic acid, Chiral pool
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.
1371 - 1377
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