213923-81-0Relevant articles and documents
CHIRAL AUXILIARIES
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Paragraph 0088; 0089; 0090, (2013/07/19)
Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.
Synthesis and structure-affinity relationships of 4-(5-Aryl-1,2,3,6-tetrahydropyridino)pyrimidine derivatives as corticotropin-releasing factor1 receptor antagonists
Kumagai, Toshihito,Okubo, Taketoshi,Kataoka-Okubo, Hiromi,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
, p. 1349 - 1355 (2007/10/03)
Recently, various non-peptide corticotropin-releasing factor1 (CRF1) receptor antagonists have been reported. Structure-affinity relationships (SARs) of non-peptide CRF1 antagonists suggest that such antagonists can be constructed of three units: a hydrophobic unit (Up-Area), a proton accepting unit (Central-Area), and an aromatic unit (Down-Area). We previously presented 4-aryl-1,2,3,6-tetrahydropyridinopyrimidine derivatives including potent CRF receptor ligands 1a and 1b and proposed that the 4-aryl-1,2,3,6-tetrahydropyridino moiety might be useful as a substituent in the Up-Area. Our interest shifted to 5-aryl-1,2,3,6-tetrahydropyridinopyrimidine derivatives 2, among which compound 2m (CRA0165) had highest affinity for CRF1 receptors (IC50=11 nM). We report here the design, synthesis and SARs of derivatives 2.
4-Tetrahydropyridylpyrimidine derivatives
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, (2008/06/13)
A 4-tetrahydropyridylpyrimidine compound represented by formula (I): wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon at