- Preparation method of flupiperidinol
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The invention belongs to the technical field of medicine preparation, and particularly relates to a preparation method of flupiperidinol. The preparation method of the fluoropiperidinol, provided by the invention, comprises the following steps of providing 4-(4-chlorphenyl)-4-piperidinol of which the purity is 99% or above, providing 4-chloro-1-(4-fluorophenyl)butan-1-one of which the purity is more than 99%, mixing the 4-(4-chlorphenyl)-4-piperidinol, 4-chloro-1-(4-fluorophenyl)butan-1-one, an alkaline substance and a catalyst, and carrying out a first substitution reaction to obtain a crudeproduct, and mixing the crude product with an organic solvent, and sequentially carrying out reflux and crystallization to obtain the flupiperidinol. The flupiperidinol prepared according to the preparation method provided by the invention has relatively high yield and purity.
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Paragraph 0089-0092; 0098-0101
(2021/03/24)
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- Synthesis of N-ω-phenylalkyl-4-(p-chlorophenyl)-piperidin-4-ol analogues with potent antiproliferative activity against HCT-116 cells
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Some opioid analogues, such as morphine and loperamide, were reported to exhibit weak antiproliferative activity against tumor cells. In a study of loperamide analogues, we found that adding an N-ω-phenylalkyl group onto the 4-arylpiperidin-4-ol unit can have important effects on the antiproliferative activity of such compounds against HCT-116 cells. We optimized the distance between the phenyl group and 4-arylpiperidin unit to promote such activity.
- Hatae, Noriyuki,Kujime, Eiko,Yano, Keigo,Kizuka, Mami,Ashida, Rina,Choshi, Tominari,Nishiyama, Takashi,Okada, Chiaki,Iwamura, Tatsunori,Yoshimura, Teruki
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p. 560 - 568
(2019/07/31)
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- CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF
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Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
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Paragraph 0828
(2016/02/21)
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- Triton B-mediated mild, convenient, and efficient method for the selective alkylation of cyclic secondary amines and thiols
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Alkylation of cyclic secondary amines, thiols, and pyridazinones has been demonstrated with alkyl halides using Triton B as base and reaction medium.
- Meshram,Reddy, B. Chennakesava,Goud, P. Ramesh
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experimental part
p. 2297 - 2303
(2009/12/01)
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- Chemokine receptor antagonists and methods of use thereof
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Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof.
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- Chemokine receptor antagonists and methods of use therefor
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Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.
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- Chemokine receptor anagonists and methods of use therefor
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Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
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- CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR
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Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.
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- Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors
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Pharmacophore-based discovery, synthesis, and structure-activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism.
- Sakamuri, Sukumar,Enyedy, Istvan J,Kozikowski, Alan P,Zaman, Wahiduz A,Johnson, Kenneth M,Wang, Shaomeng
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p. 495 - 500
(2007/10/03)
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- Synthesis of 4-substituted 4-arylpiperidines
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Several novel 4-substituted 4-arylpiperidines were synthesized. The chemistry leading to 4-(4-chlorophenyl)-4-fluoropiperidine (6), 4-azido-4-(4-chlorophenyl)piperidine (7) and 4-(4-chlorophenyl)-4-methylpiperidine (8) is described. (C) 2000 Elsevier Science Ltd.
- Harriman,Shao,Luly
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p. 8853 - 8856
(2007/10/03)
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- Substituted piperidines - Highly potent renin inhibitors due to induced fit adaptation of tile active site
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The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.
- Vieira, Eric,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Gueller, Rolf,Hirth, Georges,Maerki, Hans Peter,Mueller, Marcel,Oefner, Christian,Scalone, Michelangelo,Stadler, Heinz,Wilhelm, Maurice,Wostl, Wolfgang
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p. 1397 - 1402
(2007/10/03)
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- Synthesis and dopaminergic activity of some 3-(1,2,3,6-tetrahydro-1- pyridylalkyl)indoles. A novel conformational model to explain structure- activity relationships
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The synthesis and dopaminergic properties of a novel type of dopamine agonist is described. The number and kind of essential structural elements differ significantly from that of the rigid apomorphine-type dopamine agonists. Using standard molecular modeling techniques, a conformational model is developed proposing a U-shaped conformation which might be energetically preferred through aromatic π-π-interactions between both of the electron rich aromatic structural elements of this class of compounds. Superimposition of conformations of the lead compound 28 with apomorphine yields a novel model explaining the atypical structure-activity relationships found in this class of indolealkylamines.
- Bottcher,Barnickel,Hausberg,Haase,Seyfried,Eiermann
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p. 4020 - 4026
(2007/10/02)
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- New Compounds with Possible Pharmacological Activity
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Sixty-two new organic compounds are reported.These were prepared for testing in a variety of pharmacological screens or as chemical intermediates.None was found to be more active or less toxic than known medicinals.
- Moffett, Robert Bruce
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p. 176 - 183
(2007/10/02)
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