Department of Chemistry, Organic & Bioorganic Chemistry, University of Graz, Heinrichstrasse 28, A-8010 Graz, Austria.
Chem Commun (Camb). 2010 Aug 14;46(30):5500-2. doi: 10.1039/c0cc00585a. Epub 2010 May 11.
A straightforward, high-yielding, chemoenzymatic total synthesis of enantiopure (S)-Rivastigmine was developed using various omega-transaminases for the asymmetric amination of appropriate acetophenone precursors. Optimisation of the biotransformation allowed scale-up and the total synthesis of (S)-Rivastigmine.
开发了一种直截了当、高产、酶促化学全合成方法,通过各种ω-转氨酶对合适的苯乙酮前体进行不对称氨化反应,得到手性纯(S)-利伐斯的明。通过优化生物转化条件,实现了(S)-利伐斯的明的放大合成。