910875-39-7Relevant articles and documents
Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists
Shirai, Junya,Yoshikawa, Takeshi,Yamashita, Masayuki,Yamamoto, Yasuharu,Kawamoto, Makiko,Tarui, Naoki,Kamo, Izumi,Hashimoto, Tadatoshi,Ikeura, Yoshinori
experimental part, p. 6430 - 6446 (2011/12/01)
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.
Piperidine derivative crystal, process for producing the same, and use
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Page/Page column 45; 46, (2010/11/24)
The present invention provides a piperidine derivative having antagonistic action for tachykinin receptors and the like, a crystal thereof, and an agent for the prophylaxis or treatment of diseases including lower urinary tract disease and the like, which contains the derivative. Specifically, the present invention provides an optically active compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof.