190953-80-1Relevant articles and documents
Mechanism insights into an unexpected isomerisation reaction observed during conversion of N-benzyl piperazinones to corresponding N-benzyl thio-piperazinones
Miserazzi, Emanuele,Spotti, Mario Alessandro,Profeta, Roberto,Spada, Simone,Nalin, Arnaldo,Moro, Elisa,Andreotti, Daniele
experimental part, p. 448 - 452 (2011/03/18)
An interesting and surprising rearrangement was observed during the reaction of 4-N-benzyl piperazinone derivatives with Lawesson's reagent as a thionating agent. Investigation into the possible mechanism responsible for these results is reported herein.
BICYCLIC HETEROARYL-ALKYLENE-(HOMO)PIPERAZINONES AND THIONE ANALOGUES THEREOF, THEIR PREPARATION, AND THEIR USE OF AS SELECTIVE AGONISTS OF 5HT1-LIKE RECEPTORS
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, (2008/06/13)
A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT. sub.1-like receptors, being potent agonists of the human 5-HT 1Dα receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT 1Dα receptor subtype relative to the 5-HT 1D. beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists.