Department of Medicinal Chemistry, The Faculty of Pharmaceutical Sciences, University of Copenhagen, 2 Universitetsparken, DK-2100, Denmark.
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5431-3. doi: 10.1016/j.bmcl.2010.07.105. Epub 2010 Aug 3.
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles are synthesized using a six-step protocol. Notably, the synthesis route make use of a new and improved ring-closing methodology for the assembly of the hexahydro-pyrazino[1,2-a]indole scaffold, which is based on intramolecular C-H insertion of a carbene. The compounds act as dual serotonin 5-HT2C- and 5-HT6-ligands.
新型 7-苯硫基-1,2,3,4,10,10a-六氢吡嗪并[1,2-a]吲哚通过六步合成法得到。值得注意的是，这条合成路线使用了一种新的改进的环化方法来构建六氢吡嗪并[1,2-a]吲哚骨架，其基础是卡宾的分子内 C-H 插入反应。这些化合物是 5-羟色胺 5-HT2C-和 5-HT6-受体双重配体。
