Alex Karolin, Schwarz Nicolle, Khedkar Vivek, Sayyed Iliyas Ali, Tillack Annegret, Michalik Dirk, Holenz Jörg, Díaz José Luis, Beller Matthias
Leibniz-Institut für Katalyse e.V. an der Universität Rostock, Albert-Einstein-Str. 29a, 18059 Rostock, Germany.
Org Biomol Chem. 2008 May 21;6(10):1802-7. doi: 10.1039/b802054j. Epub 2008 Mar 31.
The synthesis of new pharmaceutically interesting 3-(2-N,N-diethylaminoethoxy)indole derivatives is described. Starting from 3-silyloxy-2-methylindoles, deprotection and in situ aminoalkylation provided 3-(2-N,N-diethylaminoethoxy)indoles in good yield. Further sulfonylation of these novel indoles gave access to potential 5-HT(6) receptor ligands.
本文描述了新型药学上有意义的3-(2-N,N-二乙氨基乙氧基)吲哚衍生物的合成。从3-硅氧基-2-甲基吲哚开始,脱保护和原位氨基烷基化以良好产率得到3-(2-N,N-二乙氨基乙氧基)吲哚。这些新型吲哚的进一步磺酰化产生了潜在的5-HT(6)受体配体。