A Short Scalable Route to (−)-α-Kainic Acid Using Pt-Catalyzed Direct Allylic Amination
作者:Ming Zhang、Kenji Watanabe、Masafumi Tsukamoto、Ryozo Shibuya、Hiroyuki Morimoto、Takashi Ohshima
DOI:10.1002/chem.201406557
日期:2015.3.2
and scalable processes to access these natural products is in high demand. Herein we report the development of a short, scalable total synthesis of (−)‐α‐kainic acid, a useful compound in neuropharmacology that is, however, limited in supply from natural resources. The synthesis features sequential platinum‐catalyzed direct allylic aminations and thermal ene‐cyclization, enabling the gram‐scale synthesis
稀缺或不可获取的天然产物的供应增加对于开发更复杂的药剂和生物工具至关重要,因此,对获取这些天然产物的原子经济,分步经济和可扩展的过程的开发提出了很高的要求。本文中,我们报告了一种短而可扩展的全合成(-)-α-海藻酸的开发,这是一种神经药理学中有用的化合物,但是自然资源的供应受到限制。该合成具有连续的铂催化的直接烯丙基胺化和热烯环化的功能,可通过6个步骤克级合成(-)-α-海藻酸,总产率为34%。