Tag: 157.2102

Synthesis, characterization, crystal structures, and the biological evaluation of 2-phenylthiazole derivatives as cholinesterase inhibitors was written by Shi, Da-Hua;Song, Meng-qiu;Ma, Xiao-Dong;Su, Jia-Bin;Wang, Jing;Wang, Xiu-Jun;Liu, Yu-Wei;Liu, Wei-Wei;Si, Xin-Xin. And the article was included in Journal of Chemical Research in 2021.HPLC of Formula: 1126-09-6 This article mentions the following:

Four 2-phenylthiazole derivatives I [R = 4-methylpiperazin-1-yl, 2-morpholin-4-yl-Et, 3,5-dimethylpiperidin-1-yl, etc.] were synthesized, characterized and evaluated as cholinesterase inhibitors. The structures of the 2-phenylthiazole derivatives were confirmed by ¹H and ¹³C NMR spectroscopy, single-crystal X-ray diffraction studies, and Hirshfeld surfaces anal. Hirshfeld surface anal. of the prepared compounds showed C-H···O intermol. interactions. The cholinesterase inhibition activities of the synthesized compounds were tested by Ellman’s method. Compound I [R = 3,5-dimethylpiperidin-1-yl] showed the best acetylcholinesterase inhibition activity with an IC₅₀ value of 8.86μM and the best butyrylcholinesterase inhibition activity with an IC₅₀ value of 1.03μM. A docking study demonstrated that the same compound interacted with the catalytic anionic site and peripheral anionic site of acetylcholinesterase and the catalytic anionic site of butyrylcholinesterase. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6HPLC of Formula: 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.HPLC of Formula: 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Direct Amidation of Esters by Ball Milling was written by Nicholson, William I.;Barreteau, Fabien;Leitch, Jamie A.;Payne, Riley;Priestley, Ian;Godineau, Edouard;Battilocchio, Claudio;Browne, Duncan L.. And the article was included in Angewandte Chemie, International Edition in 2021.Recommanded Product: 1126-09-6 This article mentions the following:

The direct mechanochem. amidation of esters RC(O)OR¹ (R = Cy, Ph, pyridin-2-yl, etc.; R¹ = Me, Et) by ball milling is described. The operationally simple procedure requires an ester, amines R²NHR³ (R² = H, Me, Et; R³ = i-Pr, Ph, 2,4,6-trimethylphenyl, etc.; R²R³ = -(CH₂)₂O(CH₂)₂-, -(CH₂)₅-, -(CH₂)₆-, etc.) and 1,2,3,4-tetrahydroquinoline, and substoichiometric KOtBu, and was used to prepare a large and diverse library of 78 amide structures RC(O)N(R²)R³ and (3,4-dihydroquinolin-1(2H)-yl)(phenyl)methanone with modest to excellent efficiency. Heteroaromatic and heterocyclic components are specifically shown to be amenable to this mechanochem. protocol. This direct synthesis platform has been applied to the synthesis of active pharmaceutical ingredients (APIs) and agrochems. as well as the gram-scale synthesis of an active pharmaceutical, all in the absence of a reaction solvent. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Recommanded Product: 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Recommanded Product: 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

P(III)-Assisted Electrochemical Access to Ureas via in situ Generation of Isocyanates from Hydroxamic Acids was written by Meng, Haiwen;Sun, Kunhui;Xu, Zhimin;Tian, Lifang;Wang, Yahui. And the article was included in European Journal of Organic Chemistry in 2021.Application of 1126-09-6 This article mentions the following:

An external oxidant-free protocol for the generation of isocyanates from hydroxamic acids assisted by trivalent phosphine under mild electrochem. conditions was reported. The process started with the anodic oxidation of hydroxamic acids, followed by reacting with phosphine to form corresponding alkoxyphosphoniums and subsequent rearrangement with the release of tri-substituted phosphine oxide as the driving force to give isocyanates, which were trapped by N-based nucleophiles to produce various ureas. This method provides a broadly applicable procedure to access isocyanate intermediates under mild electrochem. conditions. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Application of 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

ABA Type Amphiphiles with Poly(2-benzhydryl-2-oxazine) Moieties: Synthesis, Characterization and Inverse Thermogelation was written by Hahn, Lukas;Kessler, Larissa;Polzin, Lando;Fritze, Lars;Forster, Stefan;Helten, Holger;Luxenhofer, Robert. And the article was included in Macromolecular Chemistry and Physics in 2021.Related Products of 1126-09-6 This article mentions the following:

Thermoresponsive polymers are frequently involved in the development of materials for various applications. Here, polymers containing poly(2- benzhydryl-2-oxazine) (pBhOzi) repeating units are described for the first time. The homopolymer pBhOzi and an ABA type amphiphile comprising two flanking hydrophilic A blocks of poly(2-methyl-2-oxazoline) (pMeOx) and the hydrophobic aromatic pBhOzi central B block (pMeOx-b-pBhOzi-b-pMeOx) are synthesized and the latter is shown to exhibit inverse thermogelling properties at concentrations of 20 weight% in water. This behavior stands in contrast to a homolog ABA amphiphile consisting of a central poly(2-benzhydryl-2-oxazoline) block (pMeOx-b-pBhOx-b-pMeOx). No inverse thermogelling is observed with this polymer even at 25 weight%. For 25 weight% pMeOx-b-pBhOzi-b-pMeOx, a surprisingly high storage modulus of ≈22 kPa and high values for the yield and flow points of 480 Pa and 1.3 kPa are obtained. Exceeding the yield point, pronounced shear thinning is observed Interestingly, only little difference between self-assemblies of pMeOx-b-pBhOzi-b-pMeOx and pMeOx-b-pBhOx-b-pMeOx is observed by dynamic light scattering while transmission electron microscopy images suggest that the micelles of pMeOx-b-pBhOzi-b-pMeOx interact through their hydrophilic coronas, which is probably decisive for the gel formation. Overall, this study introduces new building blocks for poly(2-oxazoline) and poly(2-oxazine)-based self-assemblies, but addnl. studies will be needed to unravel the exact mechanism. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Related Products of 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Related Products of 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Discovery and rational design of 2-aminopyrimidine-based derivatives targeting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3) was written by Li, Yingxiu;Wang, Peng;Chen, Cong;Ye, Tianyu;Han, Yufei;Hou, Yunlei;Liu, Yajing;Gong, Ping;Qin, Mingze;Zhao, Yanfang. And the article was included in Bioorganic Chemistry in 2020.Computed Properties of C8H15NO2 This article mentions the following:

Herein, with the help of computer-aided drug design (CADD), the structure-based rational drug design, structure-activity relationships, and synthesis of a series of 2-aminopyrimidine derivatives that inhibit both JAK2 and FLT3 kinases was described. These screening cascades revealed that compound I [R¹ = 5-Cl] demonstrated the most inhibitory activity with IC₅₀ values of 1.8 and 0.68 nM against JAK2 and FLT3 resp. Compound I [R¹ = 5-Cl] also showed potent anti-proliferative activities against HEL (IC₅₀ = 0.84μM) and Molm-13 (IC₅₀ = 0.019μM) cell lines, but relatively weak cytotoxicity against K562 and PC-3 cell lines, which proved that it might have high target specificity. In-vitro metabolism assay, I [R¹ = 5-Cl] exhibited moderate stability in RLM (Rat Liver Microsomes) with a half-life time of 31 min. In the cellular context of Molm-13, I [R¹ = 5-Cl] induced cell cycle arrest in G1/S phase and enhanced apoptosis in a dose-dependent manner. These results indicated that I [R¹ = 5-Cl] s a promising dual JAK2/FLT3 inhibitor and worthy of further development. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Computed Properties of C8H15NO2).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Computed Properties of C8H15NO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis, characterization, crystal structures, and the biological evaluation of 2-phenylthiazole derivatives as cholinesterase inhibitors was written by Shi, Da-Hua;Song, Meng-qiu;Ma, Xiao-Dong;Su, Jia-Bin;Wang, Jing;Wang, Xiu-Jun;Liu, Yu-Wei;Liu, Wei-Wei;Si, Xin-Xin. And the article was included in Journal of Chemical Research in 2021.HPLC of Formula: 1126-09-6 This article mentions the following:

Four 2-phenylthiazole derivatives I [R = 4-methylpiperazin-1-yl, 2-morpholin-4-yl-Et, 3,5-dimethylpiperidin-1-yl, etc.] were synthesized, characterized and evaluated as cholinesterase inhibitors. The structures of the 2-phenylthiazole derivatives were confirmed by ¹H and ¹³C NMR spectroscopy, single-crystal X-ray diffraction studies, and Hirshfeld surfaces anal. Hirshfeld surface anal. of the prepared compounds showed C-H···O intermol. interactions. The cholinesterase inhibition activities of the synthesized compounds were tested by Ellman’s method. Compound I [R = 3,5-dimethylpiperidin-1-yl] showed the best acetylcholinesterase inhibition activity with an IC₅₀ value of 8.86μM and the best butyrylcholinesterase inhibition activity with an IC₅₀ value of 1.03μM. A docking study demonstrated that the same compound interacted with the catalytic anionic site and peripheral anionic site of acetylcholinesterase and the catalytic anionic site of butyrylcholinesterase. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6HPLC of Formula: 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.HPLC of Formula: 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Direct Amidation of Esters by Ball Milling was written by Nicholson, William I.;Barreteau, Fabien;Leitch, Jamie A.;Payne, Riley;Priestley, Ian;Godineau, Edouard;Battilocchio, Claudio;Browne, Duncan L.. And the article was included in Angewandte Chemie, International Edition in 2021.Recommanded Product: 1126-09-6 This article mentions the following:

The direct mechanochem. amidation of esters RC(O)OR¹ (R = Cy, Ph, pyridin-2-yl, etc.; R¹ = Me, Et) by ball milling is described. The operationally simple procedure requires an ester, amines R²NHR³ (R² = H, Me, Et; R³ = i-Pr, Ph, 2,4,6-trimethylphenyl, etc.; R²R³ = -(CH₂)₂O(CH₂)₂-, -(CH₂)₅-, -(CH₂)₆-, etc.) and 1,2,3,4-tetrahydroquinoline, and substoichiometric KOtBu, and was used to prepare a large and diverse library of 78 amide structures RC(O)N(R²)R³ and (3,4-dihydroquinolin-1(2H)-yl)(phenyl)methanone with modest to excellent efficiency. Heteroaromatic and heterocyclic components are specifically shown to be amenable to this mechanochem. protocol. This direct synthesis platform has been applied to the synthesis of active pharmaceutical ingredients (APIs) and agrochems. as well as the gram-scale synthesis of an active pharmaceutical, all in the absence of a reaction solvent. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Recommanded Product: 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Recommanded Product: 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

P(III)-Assisted Electrochemical Access to Ureas via in situ Generation of Isocyanates from Hydroxamic Acids was written by Meng, Haiwen;Sun, Kunhui;Xu, Zhimin;Tian, Lifang;Wang, Yahui. And the article was included in European Journal of Organic Chemistry in 2021.Application of 1126-09-6 This article mentions the following:

An external oxidant-free protocol for the generation of isocyanates from hydroxamic acids assisted by trivalent phosphine under mild electrochem. conditions was reported. The process started with the anodic oxidation of hydroxamic acids, followed by reacting with phosphine to form corresponding alkoxyphosphoniums and subsequent rearrangement with the release of tri-substituted phosphine oxide as the driving force to give isocyanates, which were trapped by N-based nucleophiles to produce various ureas. This method provides a broadly applicable procedure to access isocyanate intermediates under mild electrochem. conditions. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Application of 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

P(III)-Assisted Electrochemical Access to Ureas via in situ Generation of Isocyanates from Hydroxamic Acids was written by Meng, Haiwen;Sun, Kunhui;Xu, Zhimin;Tian, Lifang;Wang, Yahui. And the article was included in European Journal of Organic Chemistry in 2021.Application of 1126-09-6 This article mentions the following:

An external oxidant-free protocol for the generation of isocyanates from hydroxamic acids assisted by trivalent phosphine under mild electrochem. conditions was reported. The process started with the anodic oxidation of hydroxamic acids, followed by reacting with phosphine to form corresponding alkoxyphosphoniums and subsequent rearrangement with the release of tri-substituted phosphine oxide as the driving force to give isocyanates, which were trapped by N-based nucleophiles to produce various ureas. This method provides a broadly applicable procedure to access isocyanate intermediates under mild electrochem. conditions. In the experiment, the researchers used many compounds, for example, Ethyl piperidine-4-carboxylate (cas: 1126-09-6Application of 1126-09-6).

Ethyl piperidine-4-carboxylate (cas: 1126-09-6) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 1126-09-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem