613678-03-8Relevant articles and documents
Method for preparing 2 - amino -6 - (piperi -4 - acyl) pyridine derivative
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Paragraph 0044-0047, (2021/11/14)
The invention belongs to the technical field of drug synthesis, and particularly relates to a method for preparing 2 - amino -6 - (piperi -4 - acyl) pyridine derivatives. The ammonium salt and the alkali are adopted as raw materials, the ammonia gas in the prior art is replaced, and the danger of high-temperature high-pressure operation is avoided. The reaction condition is mild, the operation process is simple and convenient, the production cost is low, and the product has high purity and yield.
Pyridylpiperidine derivative and application thereof
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, (2020/04/22)
The invention discloses a pyridylpiperidine derivative and application thereof, and particularly relates to a novel pyridylpiperidine derivative and a pharmaceutical composition containing the compound, which can be used for activating a 5-HT1F receptor.
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1F receptor agonists: Evolution from bicyclic to monocyclic cores
Zhang, Deyi,Blanco, Maria-Jesus,Ying, Bai-Ping,Kohlman, Daniel,Liang, Sidney X.,Victor, Frantz,Chen, Qi,Krushinski, Joseph,Filla, Sandra A.,Hudziak, Kevin J.,Mathes, Brian M.,Cohen, Michael P.,Zacherl, Deanna,Nelson, David L.G.,Wainscott, David B.,Nutter, Suzanne E.,Gough, Wendy H.,Schaus, John M.,Xu, Yao-Chang
, p. 4337 - 4341 (2015/11/03)
Preclinical experiments and clinical observations suggest the potential effectiveness of selective 5-HT1F receptor agonists in migraine. Identifying compounds with enhanced selectivity is crucial to assess its therapeutic value. Replacement of the indole nucleus in 2 (LY334370) with a monocyclic phenyl ketone moiety generated potent and more selective 5-HT1F receptor agonists. Focused SAR studies around this central phenyl ring demonstrated that the electrostatic and steric interactions of the substituent with both the amide CONH group and the ketone C=O group play pivotal roles in affecting the adopted conformation and thus the 5-HT1F receptor selectivity. Computational studies confirmed the observed results and provide a useful tool in the understanding of the conformational requirements for 5-HT1F receptor agonist activity and selectivity. Through this effort, the 2-F-phenyl and N-2-pyridyl series were also identified as potent and selective 5-HT1F receptor agonists.