Koh P-F, Wang P, Huang J-M, Loh T-P
Division of Chemistry & Biological Chemistry, Nanyang Technological University, 50 Nanyang Avenue, Singapore 639798, Singapore.
Chem Commun (Camb). 2014 Aug 7;50(61):8324-7. doi: 10.1039/c4cc02645d.
An efficient synthetic route towards tosyl-protected (2S)-phenyl-3-piperidone, a common intermediate for many drugs, has been developed in 5 steps in 54% yield from biomass derived furfural. The synthetic utility of the piperidone core structure was demonstrated with the synthesis of a NK1 receptor antagonist.
已开发出一条高效合成路线，可从生物质衍生的糠醛出发，经五步反应以54%的产率合成对甲苯磺酰基保护的(2S)-苯基-3-哌啶酮，这是许多药物的常见中间体。通过合成一种NK1受体拮抗剂，证明了哌啶酮核心结构的合成实用性。
