Category: 132431-09-5

Bose, D. Subhas published the artcileBoron trifluoride promoted cleavage of benzyl carbamates, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate, the main research area is boron trifluoride promoted cleavage benzyl carbamate.

A new efficient method for the cleavage of benzyl carbamates (CBZ protective groups), e.g., I, is described that involves a hard acid (BF3.OEt2)-soft nucleophile (EtSH) system. Unlike other available methods, this combination avoids the reduction of olefins, acetylenes, imines, halides and nitro groups, or the possibility of carboxylic ester hydrolysis.

Tetrahedron Letters published new progress about Protective groups. 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bengtsson, Christoffer published the artcileDesign of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats, Category: piperidines, the main research area is preparation acetyl CoA carboxylase inhibitor quinoline.

Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Optimization led to two compounds, which exhibit potent inhibition of human ACC2, 10-fold selectivity over inhibition of human ACC1, good phys. and in vitro ADME properties and good bioavailability. X-ray crystallog. has shown this series binding in the CT-domain of ACC2 and revealed two key hydrogen bonding interactions. Both most potent compounds lower levels of hepatic malonyl-CoA in vivo in obese Zucker rats.

Bioorganic & Medicinal Chemistry published new progress about Drug bioavailability. 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Category: piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Anil Kumar, K. S. published the artcileSynthesis and identification of chiral (aminomethyl)piperidine carboxamides as inhibitor of collagen induced platelet activation, Synthetic Route of 132431-09-5, the main research area is antithrombotic anticoagulant; Aminomethylpiperidine; Antiplatelet; Collagen; Epinephrine; Pyroglutamic acid; Thrombosis.

Several chiral lactam carboxamides of (aminomethyl)piperidine were synthesized and investigated for a collagen induced in vitro anti-platelet efficacy and collagen plus epinephrine induced in vivo pulmonary thromboembolism. One compound (30 μM/kg) displayed a remarkable antithrombotic efficacy (60% protection) which was sustained for more than 24 h and points to its excellent bioavailability. Other compounds (IC50 = 6.6 μM, IC50 = 37 μM), as well as their racemic mixture (IC50 = 16 μM) significantly inhibited collagen-induced human platelet aggregation in vitro. One compound displayed a dual mechanism of action against both collagen (IC50 = 3.3 μM) and (5Z)-7-[(1R,4S,5S,6R)-6-[(1E,3S)-3-hydroxy-1-octen-1-yl]-2-oxabicyclo[2.2.1]heptyl]-4-heptenoic acid (U46619) (IC50 = 2.7 μM) induced platelet aggregation. A pharmacokinetic study indicated faster absorption, prolonged and constant systemic exposure and thereby exhibiting better therapeutic response. The synthesis of the target compounds was achieved using 5-oxo-L-proline esters (pyroglutamic acid esters) and analogs, such as 2-oxo-4-oxazolidinecarboxylic acid ester, 2-oxo-4-thiazolidinecarboxylic acid ester, (2S)-6-oxo-2-piperidinecarboxylic acid ester and morpholine analogs as reactants. The title compounds thus formed included N-[[(3S)-1-[[(2S)-1-[(4-methylphenyl)methyl]-5-oxo-2-pyrrolidinyl]carbonyl]-3-piperidinyl]methyl]carbamic acid ester and related substances, such as an epimer N-[[(3R)-1-[[(2S)-1-[(4-methylphenyl)methyl]-5-oxo-2-pyrrolidinyl]carbonyl]-3-piperidinyl]methyl]carbamic acid ester and related substances..

European Journal of Medicinal Chemistry published new progress about Anticoagulants (antithrombotic agents). 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Synthetic Route of 132431-09-5.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Prime, Michael E. published the artcileDiscovery and Structure-Activity Relationship of Potent and Selective Covalent Inhibitors of Transglutaminase 2 for Huntington’s Disease, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate, the main research area is transglutaminase inhibitor preparation; Huntington disease human structure activity.

Tissue transglutaminase 2 (TG2) is a multifunctional protein primarily known for its calcium-dependent enzymic protein crosslinking activity via iso-peptide bond formation between glutamine and lysine residues. TG2 overexpression and activity have been found to be associated with Huntington’s disease (HD); specifically, TG2 is up-regulated in the brains of HD patients and in animal models of the disease. Interestingly, genetic deletion of TG2 in two different HD mouse models, R6/1 and R6/2, results in improved phenotypes including a reduction in neuronal death and prolonged survival. Starting with phenyl-acrylamide screening hit I, the SAR of this series leading to potent and selective TG2 inhibitors is described. The suitability of the compounds as in vitro tools to elucidate the biol. of TG2 was demonstrated through mode of inhibition studies, characterization of drug like properties, and inhibition profiles in a cell lysate assay.

Journal of Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chen, Yiding published the artcileDirect Copper-Catalyzed Three-Component Synthesis of Sulfonamides, SDS of cas: 132431-09-5, the main research area is aryl heteroaryl alkenyl sulfonamide preparation; copper catalyst coupling boronic acid amine DABSO; secondary cyclic acyclic amine aniline coupling boronic acid DABSO.

Sulfonamides such as N-(phenylsulfonyl)morpholine were prepared in one step by coupling of aryl-, heteroaryl-, and alkenylboronic acids such as phenylboronic acid with cyclic and acyclic alkyl secondary amines such as morpholine and primary anilines and the bis(sulfur dioxide) complex of DABCO (DABSO) in the presence of Cu(OTf)2 and 4,4′-dimethoxy-2,2′-bipyridine in DMSO. The method was used on gram scale and was used to prepare sulfonamides from drugs and drug fragments.

Journal of the American Chemical Society published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent) (primary). 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, SDS of cas: 132431-09-5.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem