New explortion of N-(2-Aminoethyl)piperidine

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Novel bronchodilatory quinazolines and quinoxalines: Synthesis and biological evaluation

A series of heterocyclic derivatives analogous to (-)vasicinone, in which the vasicinone C-ring was replaced with alkyl chain terminated by tertiary amine was prepared. N3, C4-O, C4-S or C4-N were used as the sites of attachment. The 4-[3-(1-piperidyl)propylsulfanyl]derivatives displayed bronchodilatory effect at low micromolar concentrations on isolated rat trachea, and low toxicity both on Balb/c 3T3 mouse fibroblast cells and in mice.

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Piperidine – Wikipedia,
Piperidine | C5H4754N – PubChem

 

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One-dimensionally hydrogen-bonded silver(I) saccharinate complexes with N-(2-Aminoethyl)piperidine and N-(2-Hydroxyethyl)piperidine: Synthesis, crystal structures, FTIR and thermal studies

Two new complexes [Ag(sac)(aepip)] (1) and [Ag(sac)(hepip)] (2) have been obtained by the reaction of AgNO3 with Na(sac)¡¤2H2O (sac = saccharinate) in the presence of N-(2-aminoethyl)piperidine (aepip) and N-(2-hydroxyethyl)piperidine (hepip), and characterized by elemental analysis, IR spectroscopy, thermal analysis and single crystal X-ray diffraction. Complexes 1 and 2 crystallize in the monoclinic space group C2 and triclinic space group P1, respectively. In both complexes, silver(I) is tricoordinated. The sac ligand is N-coordinated, while aepip and hepip behave as N-N and N-O bidentate chelating ligands, respectively. The pip rings of both aepip amd hepip ligands adopt typical ‘chair’ conformation. The individual molecules are linked into one-dimensional chains by two N-H…O hydrogen bonds in 1, and one O-H…O hydrogen bond in 2. TG-DTG curves illustrated that the endothermic elimination of aepip and hepip ligands takes place in the early stages of thermal decomposition, while that of the sac moiety occurs exothermically at higher temperatures to give metallic silver.

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Piperidine – Wikipedia,
Piperidine | C5H4085N – PubChem

 

Discovery of 27578-60-5

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 27578-60-5, molecular formula is C7H16N2, introducing its new discovery., 27578-60-5

Comprising a cyclic amine group phenolphthalein monomer and its preparation method (by machine translation)

Comprising a cyclic amine group phenolphthalein monomer and its preparation method, the synthesis of monomer reaction mainly phenolphthalein in the lactonic ring and corresponding primary aliphatic amine reaction generated by the reaction of the lactam, contain different cyclic amine group phenolphthalein monomer, the series monomer containing a polymerizable diphenol group and functional cyclic amine group, its through the polycondensation reaction, quaternization and ion exchange can be prepared model negatively conductive aryl ether sulfone, polyaryl ether ketone and the like anionic polymer, the method because the ammonium group as the alkaline functional group compared with the traditional three-methylamine group has stronger alkaline and better alkali stability, so the expected preparation of properties of the negatively conductive aryl ether sulfone, polyaryl ether ketone and the like polymer material. (by machine translation)

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Piperidine – Wikipedia,
Piperidine | C5H4601N – PubChem

 

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Derivatives of 5-oxy-pyrido[2,3-b]quinoxaline-9-carboxylic acid: 1173 A tricyclic system useful for the synthesis of potential intercalators

The synthesis of a new series of 5-oxy-pyrido[2,3-b]quinoxaline-9-carboxamides 4a-i and N1,N2-Bis(5-oxy-pyrido[2, 3-b]quinoxaline-9-benzoyl)ethylenediamine (5) is reported starting from 2-chloro-3-nitropyridine. Fundamental steps of the synthetic pathway are i) preparation of 2-(3-nitro-pyridin-2-ylamino)benzoic acid (1) via copper-catalyzed condensation of 2-chloro-3-nitropyridine with o-anthranilic acid, ii) intramolecular cyclization of the acid 1 to 5-oxy-pyrido[2,3-b]quinoxaline-9-carboxylic acid (2b) upon treatment with concentrated sulfuric acid and oleum and iii) conversion of the acid 2 to the desired amides 4a-i and 5. Compounds 4a-i and 5 are oxygenated azaanalogs of phenazines, a wellknown series of intercalators with cytotoxic activity.

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Piperidine – Wikipedia,
Piperidine | C5H4142N – PubChem

 

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Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy

The nuclear protein poly(ADP-ribose) polymerase-1 (PARP-1) has a well-established role in the signaling and repair of DNA and is a prominent target in oncology, as testified by the number of candidates in clinical testing that unselectively target both PARP-1 and its closest isoform PARP-2. The goal of our program was to find a PARP-1 selective inhibitor that would potentially mitigate toxicities arising from cross-inhibition of PARP-2. Thus, an HTS campaign on the proprietary Nerviano Medical Sciences (NMS) chemical collection, followed by SAR optimization, allowed us to discover 2-[1-(4,4-difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118, 20by). NMS-P118 proved to be a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles and high efficacy in vivo both as a single agent and in combination with Temozolomide in MDA-MB-436 and Capan-1 xenograft models, respectively. Cocrystal structures of 20by with both PARP-1 and PARP-2 catalytic domain proteins allowed rationalization of the observed selectivity.

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Piperidine – Wikipedia,
Piperidine | C5H4262N – PubChem