22093-36-3Relevant academic research and scientific papers
Synthesis, pharmacological activity and structure affinity relationships of spirocyclic σ1 receptor ligands with a (2-fluoroethyl) residue in 3-position
Maestrup, Eva Gro?e,Wiese, Christian,Schepmann, Dirk,Brust, Peter,Wünsch, Bernhard
experimental part, p. 393 - 405 (2011/02/27)
In order to develop a fluorinated radiotracer for imaging of σ1 receptors in the central nervous system a series of (2-fluoroethyl) substituted spirocyclic piperidines 3 has been prepared. In the key step of the synthesis 2-bromocinnamaldehyde
Efficient synthesis of a highly selective NPY-5 receptor antagonist: A drug candidate for the treatment of obesity
Itoh, Takahiro,Kato, Shinji,Nonoyama, Nobuaki,Wada, Toshihiro,Maeda, Kenji,Mase, Toshiaki,Zhao, Matthew M.,Song, Jake Z.,Tschaen, David M.,McNamara, James M.
, p. 822 - 828 (2012/12/22)
A concise and practical synthesis of highly selective NPY-5 receptor antagonist 1 is described. The animopyrazine intermediate 3 was synthesized via either monobromination of aminopyrazine or palladium-catalyzed regioselective debromination of dibromopyrazine followed by an efficient Suzuki-Miyaura coupling. For the preparation of the spirolactone piperidine 2, significantly improved yield was achieved by using a combination of n-BuMgCl and n-BuLi. This protocol also dramatically increased the thermal stability of the aryllithium intermediate and eliminated the requirement for costly cryogenic conditions. The union of the spirolactone piperidine 2 and aminopyrazine 3 via a carbonyl group was accomplished using phenyl chloroformate delivering the target molecule in high yield.
Benzimidazolidinone derivatives as muscarinic agents
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Page/Page column 38, (2010/02/06)
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
Pyrazole compounds, pharmaceutical compositions, and methods for modulating or inhibiting ERAB or HADH2 activity
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, (2008/06/13)
Pyrazole compounds represented by the formula: are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in treating ERAB, HADH2 or amyloid-β mediated diseases and conditions
