Some scientific research about Ethyl N-Boc-4-methylpiperidine-4-carboxylate

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Facile synthesis of 4-substituted-4-aminopiperidine derivatives, the key building block of piperazine-based CCR5 antagonists

4-Substituted-4-aminopiperidine is an interesting structural motif found in a number of bioactive compounds. An efficient and convenient method for the synthesis of 4-differently substituted-4-aminopiperidine derivatives was described, employing isonipecotate as a starting material and Curtius rearrangement as a key step. The alkylation of isonipecotate could introduce various substituents at the 4-position of the piperidine ring. With this key building block, we are able to efficiently synthesize piperazino-piperidine based CCR5 antagonist in a highly convergent manner free of using toxic reagents such as diethylaluminum cyanide. The concise synthesis of a potent bioavailable CCR5 antagonist as HIV-1 entry inhibitor, Sch-350634 (1) was accomplished in excellent yield using N?-Boc-4-methyl-4-aminopiperidine 5a as a smart building block. The new methodology provides a facile and practical access to the piperazino-piperidine amide analogs as HIV-1 entry inhibitors.

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Piperidine – Wikipedia,
Piperidine | C5H21913N – PubChem

 

Top Picks: new discover of Piperidine-2,6-dione

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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, 1121-89-7, name is Piperidine-2,6-dione, introducing its new discovery. HPLC of Formula: C5H7NO2

Synthesis and preliminary anticancer study of 5-fluorouracil-phthalimide conjugate utilizing molecular hybridization approach

Cancer is still the most challenging disease in the entire world. Molecular hybridization is very interesting approach in design of drug and development depends on the combination of pharmacophoric moieties of two pharmacologically active compounds results in a new hybrid compound with better affinity and efficacy, when compared to the parent drugs. The aim of the present study is to synthesize new 5-fluorouracil derivatives as probable more active anticancer agents than the parent drug. 5-fluoro-4-oxo-1,4-dihydropyrimidin-2-yl2-(1,3-dioxoisoindolin-2-ylamino) acetate [IV] and 2-(2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-oxoethylamino) isoindoline-1,3-dione [V] have been synthesized utilizing hybridization approach from 5-fluorouracil and phthalimide through amino acetate or 2-oxoethylamino linkers. The structures of the newly synthesized compounds and their intermediates were characterized by FT-IR,13C-NMR ESI-MS spectral analysis. A preliminary cytotoxicity study that evaluated by crystal violet assay using a target breast cancer cell, murine mammary adenocarcinoma cell line indicates that the compounds have considerable anticancer activity relative to the lead one.

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Piperidine – Wikipedia,
Piperidine | C5H1472N – PubChem

 

Can You Really Do Chemisty Experiments About 42538-31-8

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NEW CHIRAL AMINOPHOSPHINES PREPARED FROM L-ORNITHINE AND CATALYTIC ASYMMETRIC HYDROGENATION USING THEIR RHODIUM(I) COMPLEXES

From readily preparable chiral diamines were obtained new aminophosphines, (3S)--3-aminopiperidine, and (3S)--3-(methylamino)piperidine.Asymmetric hydrogenation of alpha-acylaminoacrylic acids, employing Rh(I) complexes with these aminophosphines as catalyst, gave optically active N-acyl-alpha-amino acids.

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Piperidine | C5H8311N – PubChem

 

Awesome and Easy Science Experiments about 1-Phenylpiperidine-4-carbaldehyde

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A Novel Highly Stereoselective Synthesis of Tetrahydrodibenzo-1,4-dioxanes

The cis- and trans-tetrahydrodibenzo-1,4-dioxanes 2 and 3 were synthesized from 2-bromocyclohexanone in five steps. – Key Words: Dichotomy in SN2 reactions / 1,4-Benzodioxanes, potential biological activity of

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Piperidine | C5H11714N – PubChem

 

Awesome Chemistry Experiments For 177-11-7

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Safety of 1,4-Dioxa-8-azaspiro[4.5]decane, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 177-11-7, Name is 1,4-Dioxa-8-azaspiro[4.5]decane, molecular formula is C7H13NO2. In a Article, authors is Guerrero, Miguel£¬once mentioned of 177-11-7

Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140)

kappa opioid receptor (KOR) antagonists are potential pharmacotherapies for the treatment of migraine and stress-related mood disorders including depression, anxiety, and drug abuse, thus the development of novel KOR antagonists with an improved potency/selectivity profile and medication-like duration of action has attracted the interest of the medicinal chemistry community. In this paper, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4 amine (CYM-53093, BTRX-335140) as a potent and selective KOR antagonist, endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments. Orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. This compound is in phase 1 clinical trials for the treatment of neuropsychiatric disorders wherein dynorphin is thought to contribute to the underlying pathophysiology.

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Piperidine | C5H7553N – PubChem

 

More research is needed about tert-Butyl piperidin-4-ylcarbamate

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SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1, 2-A]PYRIDINE-3- CARBOXAMIDE COMPOUNDS AS CFMS INHIBITORS

Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.

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Piperidine | C5H14312N – PubChem

 

Some scientific research about 1121-89-7

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DIELS-ALDER REACTIONS OF 2-AZADIENES. DIASTEREOSELECTIVE SYNTHESES OF 2-AZABICYCLO<2.2.2>OCTAN-2-ONES AND OF 2,3,4-SUBSTITUTED CYCLOHEXANONES

Glutarimide is readily disilylated to yield the cyclic 2-azadiene 1 which reacts with open-chain dienophiles with surprisingly high exo-selectivity.The resulting 2-aza-bicyclo<2.2.2>octan-3-ones are stereoselectively transformed into substituted cyclohexanones.

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Piperidine | C5H1429N – PubChem

 

Simple exploration of 138022-02-3

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Fused imidazopyridine derivatives as antihyperlipidemic agents

A novel compound of the formula: wherein ring Q is an optionally substituted pyridine ring;One of R0, R1 and R2 is ?Y0?Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group;Y0 is a bond or an optionally substituted bivalent hydrocarbon group;Z0 is a basic group which may be bonded via oxygen, nitrogen, ?CO?, ?CS?, ?SO2N(R3)? (where R3 is hydrogen or an optionally substituted hydrocarbon group), or S(O)n (wherein n is to 0, 1 or 2);………is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.

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Extracurricular laboratory:new discovery of 3-(1-(tert-Butoxycarbonyl)piperidin-4-yl)propanoic acid

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PYRROLIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to pyrrolidine compounds of the formula 1: (wherein R 1, R 2, R 3, R 4, R 5, R 6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

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Piperidine | C5H21144N – PubChem

 

Simple exploration of 1,4-Dioxa-8-azaspiro[4.5]decane

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Erythropoietin mimetics derived from solution phase combinatorial libraries

The erythropoietin receptor (EPOr) is activated by ligand-induced homodimerization, which leads to the proliferation and differentiation of erythroid progenitors. Through the screening of combinatorial libraries of dimeric iminodiacetic acid diamides, novel small molecule binders of EPOr were identified in a protein binding assay. Evaluation of a series of analogues led to optimization of binding subunits, and these were utilized in the synthesis of higher order dimer, trimer, and tetramer libraries. Several of the most active EPOr binders were found to be partial agonists and induced concentration-dependent proliferation of an EPO-dependent cell line (UT-7/EPO) while having no effect on a cell line lacking the EPOr (FDC-P1). An additional compound library, based on a symmetrical isoindoline-5,6-dicarboxylic acid template and including the optimized binding subunits, was synthesized and screened leading to the identification of additional EPO mimetics.

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Piperidine – Wikipedia,
Piperidine | C5H7432N – PubChem