Cu(OAc) 2 -catalyzed regioselective oxidative C-H cyanation of two different types of aromatics was described, providing facile access to functionalized heterocycles in good yields. Control experiments suggest the copper chelation-assisted oxidative C-H activation mechanism.

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.

Title compound (II), key building block for the synthesis of the first‐in‐class Janas tyrosine kinase inhibitor CP‐690,550, is prepared from cheap raw materials using established transformations.

A Novel Asymmetric Synthesis of cis-(3R,4R)-N-(tert-Butoxycarbonyl)-4-methyl-3-(methylamino)piperidine A s y m m e t r i c S y n t h e s i s o f a K e y P i p e r i d i n e D e r i v a t i v e Abstract: cis-(3R,4R)-N-(tert-Butoxycarbonyl)-4-methyl-3-(methylamino)piperidine, a key intermediate for the synthesis of CP-690550 (a potent protein kinase inhibitor), is prepared via an asymmetric approach starting from ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride in an overall yield of 49%. The mild conditions and high yields obtained during the synthesis suggest a potential industrial application for this route.