16727-34-7Relevant academic research and scientific papers
5(10→9)abeo-ergoline derivatives: Synthesis, 5-HT(1A)-receptor affinity and selectivity
Mantegani, Sergio,Baumer, Luca,Brambilla, Enzo,Caccia, Carla,Fornaretto, Maria Gioia,McArthur, Robert Albert,Varasi, Mario
, p. 279 - 292 (2007/10/03)
The synthesis and the structure-affinity relationship (S.A.F.I.R.) study for the 5-HT(1A) receptor sites of a novel series of 5(10→9)abeo-ergoline derivatives are presented. Most derivatives showed moderate to high affinity and selectivity for 5-HT(1A) receptor sites. The structure-affinity relationship pointed out the role of the substituent at position 8, and the outstanding importance of the reduction of the indole 2,3-double bond for achieving the highest 5-HT(1A) affinity and selectivity within the compounds presented.
Synthesis of 5(10→9)abeo-ergolines
Mantegani, Sergio,Arlandini, Emanuele,Borghi, Daniela,Brambilla, Enzo,Varasi, Mario
, p. 1493 - 1506 (2007/10/03)
Reaction of the (5 R, 8 R)-ergoline derivative (6) with the couple CCl4/(Ph)3P unexpectedly resulted in the formation of the novel (5 S, 8 R)-5 (10→9)abeo-ergoline derivative. A mechanism of this transposition process is proposed.
