## Abstract A variety of novel 7‐sulfanylpyrazinoindole derivatives (V) (11 examples) is synthesized using a new and improved ring‐closing methodology for the assembly of the hexahydropyrazinol[1,2‐α]indole scaffold.
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands
✍ Scribed by N. Krogsgaard-Larsen; A.A. Jensen; J. Kehler
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 268 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]
indoles are synthesized using a sixstep 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-HT 2C -and 5-HT 6 -ligands.
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## Abstract The synthesis of [^3^H]CP‐96,501 [5‐(2,3‐ditritiopropoxy)‐3‐(1,2,5,6‐tetrahydropyrid‐4‐yl)indole], a selective radioligand for the serotonin (5‐HT~1B~) receptor and analog of RU‐24,969, is described. 5‐Hydroxyindole is converted in two steps to 5‐(2‐propenyloxy)‐3‐(N‐__t__‐butoxycarbony