- A methanesulfonic acid pu vertical preparation method
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The invention discloses a preparation method of pridinol mesylate. The preparation method comprises the following steps: carrying out reaction on methyl acrylate and piperidine to obtain methyl 3-(1-piperidyl) propionate, carrying out reaction on methyl 3-(1-piperidyl) propionate and phenyl magnesium bromide (as a Grignard reagent) to obtain pridinol, and forming a salt by pridinol and methanesulfonic acid in a solvent such as an ether solvent to obtain pridinol mesylate as a final product. The process route is simple in synthetic steps, is short in reaction route, is high in yield and is economical and practical.
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Paragraph 0018; 0019; 0020
(2017/06/02)
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- Synthesis of 4-arylpiperidin-4-ol derivatives of loperamide as agents with potent antiproliferative effects against HCT-116 and HL-60 cells
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The structure of 4-arylpiperidin-4-ol, a constituent of the antidiarrheal loperamide, is key to μ opioid receptor activation. Some opioid derivatives were recently reported to induce tumor cell death, but the chemical structures responsible for their antitumor activity remain unclear. We synthesized loperamide analogs and tested their antiproliferative activity against HCT-116 colon tumor cells and HL-60 leukemia cells. The N-substituents on 4-arylpiperidin-4-ol units were found to play an important role in their antiproliferative activity, and the N-diphenylpropanol analogs exhibited the most potent antiproliferative activity. Furthermore, the N-diphenylpropanol analog activated caspase-3, as was found previously for opioids that exhibited antitumor effects.
- Hatae, Noriyuki,Nagayama, Tomoyuki,Esaki, Hiroyoshi,Kujime, Eiko,Minami, Masabumi,Ishikura, Minoru,Choshi, Tominari,Hibino, Satoshi,Okada, Chiaki,Toyota, Eiko,Nagasawa, Hideko,Iwamura, Tatsunori
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p. 663 - 673
(2016/11/13)
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- Tuning the reducing properties of 1,2-diaryl-1,2-disodiumethanes
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(Chemical Equation Presented) We investigated the reducing properties of a series of 1,2-diaryl-1,2-disodiumethanes by means of equilibration reactions. The electron-donor power of these vic-diorganometals is strongly affected by the nature of substituents present either on the aromatic ring(s) or on the carbanionic centers, and it can be correlated with their ability to delocalize the arylmethyl carbanions. These findings are supported by electrochemical analysis of the reduction behavior of the parent 1,2-diarylalkene. Applications of these results to the reduction of selected substrates are described. 2009 American Chemical Society.
- Azzena, Ugo,Pisano, Luisa,Antonello, Sabrina,Maran, Flavio
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supporting information; experimental part
p. 8064 - 8070
(2010/03/02)
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- Simple synthetic equivalents for the β-(N,N-disubstituted)ethylamino acyl cation synthon and their applications
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Various N,N-disubstituted-β-amino-N-methoxy-N-methylpropanamides 3a-i were prepared which served as an excellent β-aminoacyl cation equivalents. These were used to prepare β-amino ketones 1, pharmacologically active tertiary 1-(3,3-diarylpropyl)amines 7a-c, and the interesting C-glycoside 8.
- Selvamurugan,Aidhen
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p. 2239 - 2246
(2007/10/03)
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