Development of κ opioid receptor agonists by focusing on phenyl substituents of 4-dimethylamino-3-phenylpiperidine derivatives: Structure-activity relationship study of matrine type alkaloids
A series of new κ opioid receptor (KOR) agonists were developed from the lead compound 4-dimethylamino-1-pentanoylpiperidine (3), a matrine-type alkaloid. Derivatives of 3 were synthesized with a variety of phenyl substituents and evaluated for their anti
Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists
We synthesized a series of novel 3-phenyl-4-benzylaminopiperidine derivatives that were identified as potent tachykinin NK1 receptor antagonists by structural modification of the 3-benzhydrylpiperidone derivative through high-throughput screening. N-{2-[(3R,4S)-4-({2-Methoxy-5-[5-(trifluoromethyl)- 1Htetrazol-1-yl]benzyl}amino)-3-phenyl-1-piperidinyl]-2-oxoethyl}acetamide ((+)-39) was found to be one of the most potent tachykinin NK1 receptor antagonists with high metabolic stability. Highly efficient asymmetric synthesis of (+)-39 was achieved via dynamic kinetic resolution.
Synthesis of 3-phenyl-4-piperidones from acetophenone by shapiro and azamichael reactions and their further derivatization
The Shapiro reaction of acetophenone is the key in a convenient three-step access to a divinyl ketone which is further transformed by double aza-Michael reactions with primary amines into N-substituted 3-phenyl-4-piperidones. In the case of N-benzyl and N
Rosiak, Anna,Hoenke, Christoph,Christoffers, Jens
p. 4376 - 4382
(2008/04/13)
PIPERIDINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
The present invention provides a compound represented by the formula: ???wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydroca
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Page/Page column 43
(2008/06/13)
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