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AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS

The present invention is directed to novel aminopyrrolidines of formula I, pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12798N – PubChem

 

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 58333-75-8 is helpful to your research. Computed Properties of C12H17NO

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 58333-75-8, name is 4-(2-Methoxyphenyl)piperidine, introducing its new discovery. Computed Properties of C12H17NO

Benzimidazoles that are useful in treating sexual dysfunction

The present invention relates to the use of compounds of formula (I) 1 for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12789N – PubChem

 

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Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D3 receptor agonists

The dopamine D3 receptor (D3R) is a proven therapeutic target for the treatment of neurological and neuropsychiatric disorders. In particular, D3R-selective ligands that can eliminate side effects associated with dopamine D2 receptor (D2R) therapeutics have been validated. However, the high homology in signaling pathways and the sequence similarity between D2R and D3R have rendered the development of D3R-selective ligands challenging. Herein, we designed and synthesized a series of piperazine-phthalimide bitopic ligands based on a fragment-based and molecular docking inspired design. Compound 9i was identified as the most selective D3R ligand among these bitopic ligands. Its selectivity was improved compared to reference compounds 1 and 2 by 9- and 2-fold, respectively, and it was 21-fold more potent than compound 2. Molecular docking demonstrated that the orientation of Leu2.64 and Phe7.39 and the packing at the junction of helices may affect the specificity for D3R over D2R. Functional evaluation revealed that D3R-selective ligand 9i displayed a subpicomolar agonist activity at D3R with a 199-fold increase in potency compared to quinpirole. These results may be useful for the fragment-based design of bitopic compounds as selective D3R ligands.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12803N – PubChem

 

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58333-75-8, 4-(2-Methoxyphenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

58333-75-8, 4-(2-Methoxyphenyl)piperidine (200 mg, 1 mmol), the product from Example 1A (228 mg, 1 mmol) and N,N-diisopropylethylamine (0.185 mL, 1.1 mmol) in toluene (8 mL) were stirred at 60 C. for 18 hours. The reaction mixture was poured into water (30 mL) and extracted with ethyl acetate (30 mL). The organic layer was washed with brine (230 mL), dried over MgSO4, filtered and the filtrate concentrated under reduced pressure. The residue was purified by flash chromatography on silica gel (elution with dichloromethane:methanol, 9.5:0.5) to provide the title compound 177 mg (52.3%). 1H NMR (300 MHz, DMSO-d6) ? 1.71 (m, 4H), 2.28 (m, 5H), 2.89 (m, 1H), 2.96 (m, 2H), 3.13 (s, 2H), 3.78 (s, 3H), 6.91 (m, 3H), 7.20 (m, 3H), 7.45 (m, 2H), 8.69 (s, 1H); MS (DCI/NH3) m/e 339 (M+H)+. Anal. calcd for C21H26N2O2: C, 74.52; H, 7.74; N, 8.28. Found: C, 74.23, H, 7.71, N, 8.26.

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Reference£º
Patent; Stewart, Andrew O.; Kolasa, Teodozyj; US2003/232836; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

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58333-75-8, 4-(2-Methoxyphenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 26 mmol 4-(2-methoxyphenyl)-piperidine (Maybridge) in 100 ml dry DICHLOROMETHANE were added 28.6 mmol triethylamine and 78 mmol ETHYLCHLOROFONNATE at 0 The solution was stirred at room temperature overnight, washed twice with 0.5 M HC1 (125 ml) then dried over MGS04 and evaporated. The product was sufficiently pure to be used in the following steps.

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Reference£º
Patent; H. LUNDBECK A/S; WO2004/87155; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

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The synthetic route of 58333-75-8 has been constantly updated, and we look forward to future research findings.

58333-75-8, 4-(2-Methoxyphenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 21 2-{[4-(2-methoxyphenyl)piperidin-1-yl]methyl}-1H-benzimidazole A mixture of 4-(2-methoxyphenyl)piperidine (0.2 g, 1.06 mmol), 2-chloromethyl-benzimidazole (186, 1.1 mmol) and Cs2CO3 (0.36 g, 0.36 mmol) in DMF (8 mL) were stirred at room temperature for 18 hours. The reaction mixture was poured into water (30 mL) and extracted with ethyl acetate (20 mL). The organic layer was washed with brine (2*30 mL) and dried over MgSO4, filtered and the filtrate concentrated under reduced pressure. The residue was purified by flash chromatography eluding with 5% methanol in dichloromethane to give the title compound (82 mg, 25%). 1H NMR (CDCl3, 300 MHz) delta 1.69 (m, 4H), 2.19 (m, 2H), 2.87(m, 1H), 2.96 (m, 2H), 3.75 (s, 2H), 3.77 (s, 3H), 6.92 (m, 2H), 7.45 (m, 1H), 7.55 (m, 1H), 12.26 (s, 1H). MS (DCI-NH3) m/z 322 (M+H)+.

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Reference£º
Patent; Abbott Laboratories; US6960589; (2005); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem