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Paper | Regular issue | Vol 24, No. 11, 1986, pp.3105-3114
Published online, 1st January, 1970
DOI: 10.3987/R-1986-11-3105
Synthesis and Pharmacological Activity of C(1)- and N(2)-Substituted β-Carboline Derivatives

Ralf Plate, Rutger J. F. Nivard, Harry C. J. Ottenheijm,* Julianna Kardos, amd Miklos Simotyi

*Department of Organic Chemistry, University of Nijmegen, Toernooiveld, 6525 ED Nijmegen, The Netherlands


A series of C(1) as well as N(2)-hetero-substituted β-carbolines has heen synthesized from indoles via N-hydroxytryptophan derivatives (Schemes I and II). Preliminary pharmacodynamical data are provided (Tabel I). Of the β-carbolines 4,5,14-16 prepared, the compounds 4,5 and 14 show appreciable in vitro affinity towards the benzodiazepine receptor.