58879-07-5Relevant academic research and scientific papers
Synthesis method for (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine and synthesis method for chiral intermediate of niraparib
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Paragraph 0083-0090, (2018/07/10)
The invention belongs to the technical field of organic synthesis. The synthesis method firstly provided by the invention takes benzyl-4-oxopiperidine as a starting material, and the starting materialis subjected to Grignard reaction, elimination reaction, hydrogenation reduction reaction and chiral resolution in sequence to successfully obtain a target product (R)-3-phenylpiperidine or/ and (S)-3-phenylpiperidine. The synthesis method sencondly provided by the invention takes the same starting raw material for Grignard reaction, organic silicon reagent is used for removing a hydroxide radical, and benzyl is removed by catalytic hydrogenation reaction; finally, the chiral resolution is carried out to obtain a target product. The (S)-3-phenylpiperidine can be synthesized according to the synthesis method. (S)-3-p-aminosalicylic phenylpiperidine can be synthesized according to the third aspect; or according to the fourth aspect, (S)-3-p-bromophenyl piperidine is synthesized to serve asthe key intermediate for preparing the niraparib. According to the synthesis method for (R)-3-phenylpiperidine or/ and (S)-3-phenylpiperidine and the synthesis method for chiral intermediate of niraparib, production cost is obviously lowered, and the synthesis methods are favorable for the large-scale industrial production of a niraparib medicine.
Novel piperidyl derivatives of quinazoline and isoquinoline
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Page/Page column 22, (2010/02/15)
The invention pertains to new piperidyl-substituted quinazoline and isoquinoline derivatives that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders.
Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists
Wang, Xueqing,Bhatia, Pramila A.,Daanen, Jerome F.,Latsaw, Steve P.,Rohde, Jeffrey,Kolasa, Teodozyi,Hakeem, Ahmed A.,Matulenko, Mark A.,Nakane, Masaki,Uchic, Marie E.,Miller, Loan N.,Chang, Renjie,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
, p. 4667 - 4678 (2007/10/03)
A series of 3-aryl piperidine analogs with 2-piperidinoalkylamino or 2-piperidinoalkyloxy fused bicyclic rings were prepared and found to be potent and efficacious human dopamine D4 agonists. The synthesis and structure-activity relationship (SAR) studies that led to the identification of these compounds are discussed.
Subtype-selective NMDA receptor ligands and the use thereof
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, (2008/06/13)
The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neuro-degenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
An efficient synthesis of N-aroyl-3-phenyltetrahydropyridines
Sui, Zhihua,Dodd, John,Ohemeng, Kwasi A.
, p. 175 - 185 (2007/10/03)
N-Aroyl-3-phenyltetrahydropyridines were conveniently synthesized by dehydration of N-aroyl-3-hydroxy-3-phenylpiperidines with toluenesulfonic acid on silica gel as a dehydration reagent.
