- Efficient copper-catalyzed cross-coupling of 1-Boc-piperazine with aryl iodides and its application in the synthesis of trazodone
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A convenient and practical strategy is developed for the cross-coupling of N-Boc protected piperazines with aryl iodides using CuBr/1,1′-bi-2- naphthol as the catalyst and K3PO4 as the base. The protocol affords N-arylated piperazine products in moderate to good yields under the optimized conditions. The application of this catalytic system to the synthesis of trazodone is also successfully demonstrated using commercially available substrates.
- Yong, Fui-Fong,Teo, Yong-Chua,Tan, Khee-Ngiap
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p. 5332 - 5334
(2013/09/12)
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- Synthesis of new piperazine-pyridazinone derivatives and their binding affinity toward α1-, α2-adrenergic and 5-HT1A serotoninergic receptors
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We report the design and synthesis of a new class of piperazine- pyridazinone analogues. The arylpiperazine moiety, the length of the spacer, and the terminal molecular fragment were varied to evaluate their influence in determining the affinity of the new compounds toward the α1- adrenergic receptor (α1-AR), α2-adrenergic receptor (α2-AR), and the 5-HT1A serotoninergic receptor (5-HT1AR). Biological data showed that most of the compounds have an α1-AR affinity in the nanomolar or subnanomolar range, while affinity toward the other two receptors was lower in most cases. However, several of the tested compounds also showed very good (in the nanomolar range) or moderate affinity toward the 5-HT1AR subtype.
- Betti, Laura,Zanelli, Marco,Giannaccini, Gino,Manetti, Fabrizio,Schenone, Silvia,Strappaghetti, Giovannella
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p. 2828 - 2836
(2007/10/03)
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- [(3-Chlorophenyl)piperazinylpropyl]pyridazinones and analogues as potent antinociceptive agents
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A number of [(3-chlorophenyl)piperazinylpropyl]pyridazinones and the corresponding isoxazolopyridazinones, showing the arylpiperazinyl substructure present in very potent antinociceptive agents reported in the literature, were synthesized and tested for t
- Giovannoni, Maria Paola,Vergelli, Claudia,Ghelardini, Carla,Galeotti, Nicoletta,Bartolini, Alessandro,Dal Piaz, Vittorio
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p. 1055 - 1059
(2007/10/03)
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