1233955-69-5Relevant articles and documents
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist
Li, Xin,Wan, Hong,Dong, Ping,Wang, Bin,Zhang, Lei,Hu, Qiyue,Zhang, Ting,Feng, Jun,He, Feng,Bai, Chang,Zhang, Lianshan,Tao, Weikang
supporting information, p. 2151 - 2155 (2020/12/17)
Analgesics with no abuse liability are highly demanded in the market. KOR agonists have been proved to be strong analgesics without MOR agonist-related side effects, such as respiratory depression, tolerance, and dependence liability; however, activation
Synthesis method of 1-methyl-3-(piperidine-4-yl) urea hydrochloride
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Paragraph 0029; 0032; 0038; 0044, (2017/07/22)
The invention relates to a synthesis method of 1-methyl-3-(piperidine-4-yl) urea hydrochloride. The synthesis method comprises the following steps: (1) reacting N-Boc-4-aminopiperidine with methylchloroformate in a solvent in the presence of organic alkali to generate N-Boc-4-[(methoxy acyl) amino] piperidine; (2) reacting N-Boc-4-[(methoxy acyl) amino] piperidine prepared in the step (1) with methylamine in the solvent in the presence of organic alkali to generate 1-methyl-3-(N-Boc-piperidine-4-yl) urea; and (3) reacting 1-methyl-3-(N-Boc-piperidine-4-yl) urea prepared in the step (2) with acetyl chloride in the solvent to obtain a final product which is 1-methyl-3-(piperidine-4-yl) urea hydrochloride. The method is easily available in raw materials, mild in reaction condition, easy to operate and high in total yield; the molar total yield of three steps of reaction, which is metered according to the raw material N-Boc-4-aminopiperidine, can reach not less than 87%; the method is applicable to industrial production.
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N- (benzyloxycarbonyl)amino)piperidin-1-yl)butanes
Finke, Paul E.,Oates, Bryan,Mills, Sander G.,MacCoss, Malcolm,Malkowitz, Lorraine,Springer, Martin S.,Gould, Sandra L.,DeMartino, Julie A.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Schleif, William A.,Emini, Emilio A.
, p. 2475 - 2479 (2007/10/03)
(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro (2,3-dihydrobenzthiophene-3,4′-piperidin-1′-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50 = 10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of 4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists.