Tag: 155.2804

Design and Synthesis of High Affinity Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferases Directed by Ligand Efficiency Dependent Lipophilicity (LELP) was written by Rackham, Mark D.;Brannigan, James A.;Rangachari, Kaveri;Meister, Stephan;Wilkinson, Anthony J.;Holder, Anthony A.;Leatherbarrow, Robin J.;Tate, Edward W.. And the article was included in Journal of Medicinal Chemistry in 2014.Computed Properties of C10H21N This article mentions the following:

N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. We have previously reported that 2-(3-(piperidin-4-yloxy)benzo[b]thiophen-2-yl)-5-((1,3,5-trimethyl-1H-pyrazol-4-yl)methyl)-1,3,4-oxadiazole (34c) is a high affinity inhibitor of both Plasmodium falciparum and P. vivax NMT and displays activity in vivo against a rodent malaria model. Here we describe the discovery of 34c through optimization of a previously described series. Development, guided by targeting a ligand efficiency dependent lipophilicity (LELP) score of less than 10, yielded a 100-fold increase in enzyme affinity and a 100-fold drop in lipophilicity with the addition of only two heavy atoms. 34c was found to be equipotent on chloroquine-sensitive and -resistant cell lines and on both blood and liver stage forms of the parasite. These data further validate NMT as an exciting drug target in malaria and support 34c as an attractive tool for further optimization. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Computed Properties of C10H21N).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Computed Properties of C10H21N

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Differences in Al distribution and acidic properties between RTH-type zeolites synthesized with OSDAs and without OSDAs was written by Liu, Ming;Yokoi, Toshiyuki;Yoshioka, Masato;Imai, Hiroyuki;Kondo, Junko N.;Tatsumi, Takashi. And the article was included in Physical Chemistry Chemical Physics in 2014.Application of 79-55-0 This article mentions the following:

In addition to the original preparation route of the RTH-type zeolites using 1,2,2,6,6-pentamethylpiperidine (PMP) as an organic structure directing agent (OSDA), simpler organic amines such as N-methylpiperidine and pyridine can be used as alternative OSDAs in place of PMP. Also, the authors established a synthesis method for preparing the RTH-type zeolites without using any OSDAs. RTH-type aluminosilicates were synthesized with different types of OSDA or without using any OSDAs. The obtained zeolites synthesized with different preparation methods were characterized by using various techniques, especially high-resolution ²⁷Al MASNMR and in situ FTIR techniques using CO adsorption. The relation between the preparation method and the catalytic performance in the methanol to olefins (MTO) reaction was discussed. Finally, the distribution of Al species in the RTH-framework was clarified. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Application of 79-55-0).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 79-55-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Transition metal-free methylation of amines with formaldehyde as the reductant and methyl source was written by Man, Nikki Y. T.;Li, Wanfang;Stewart, Scott G.;Wu, Xiao-Feng. And the article was included in Chimia in 2015.Application of 79-55-0 This article mentions the following:

A simple transition metal-free procedure using formaldehyde for the N,N-dimethylation and N-methylation of primary and secondary anilines is reported. The reaction showed limitations on sterically hindered and electron-withdrawing anilines, but is successful on amines with electron-donating substituents. Formaldehyde acts as both the reducing agent and the carbon source in the reaction. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Application of 79-55-0).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application of 79-55-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

From Zn(C₆F₅)₂ to ZnEt₂-based Lewis Pairs: Significantly Improved Catalytic Activity and Monomer Adaptability for the Ring-opening Polymerization of Lactones was written by Wang, Bin;Wei, Yuan;Li, Zong-Jun;Pan, Li;Li, Yue-Sheng. And the article was included in ChemCatChem in 2018.HPLC of Formula: 79-55-0 This article mentions the following:

In this contribution, the structure-reactivity relationships of ZnR₂/DMAP (R=C₆F₅, C₆H₅ and C₂H₅) Lewis pairs in ring-opening polymerization (ROP) of lactones were investigated by crystallog. anal., d. functional theory (DFT) calculations and kinetic studies. With decrease of ZnR₂ Lewis acidity, the interaction between ZnR₂ and DMAP weakens and the dissociation of ZnR₂路2DMAP Lewis adducts become easier, which facilitates the activation of cyclic ester monomers. Thus, the ZnEt₂/DMAP Lewis pair, bearing weakest interaction between Lewis acid and Lewis base, exhibits high catalytic activity and broad monomer adaptability. ZnEt₂路2DMAP can convert lactide (LA) rapidly into polylactide (PLA) even at room temperature Furthermore, a wide range of cyclic esters can also be polymerized using this dual catalyst, from small lactones such as 尾-butyrolactone (尾-BL), 未-valerolactone (未-VL) and 蔚-caprolactone (蔚-CL) to the strainless macrolactone. The optimal reaction pathway, key species and active species in the ZnEt₂路2DMAP catalytic ROP of LA were figured out by DFT calculations The results clearly indicated that a DMAP-LA exchange was necessary for activation of monomer, and the single mol. initiation is preferred. Meanwhile, the cyclic active species is more stable than the linear analogs, in which DMAP and ZnEt₂ bond with each polymer chain end resp. and ZnEt₂ interact with DMAP. The DFT calculation gives an account for the formation of the cyclic polyester in the ROP of LA by ZnR₂-based Lewis pairs. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0HPLC of Formula: 79-55-0).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 79-55-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

B(C₆F₅)₃-Catalyzed C-H Alkylation of N-Alkylamines Using Silicon Enolates without External Oxidant was written by Chan, Jessica Z.;Chang, Yejin;Wasa, Masayuki. And the article was included in Organic Letters in 2019.Quality Control of 1,2,2,6,6-Pentamethylpiperidine This article mentions the following:

An efficient method for the coupling of N-alkylamines with silicon enolates to generate 尾-amino carbonyl compounds is disclosed. These reactions proceed by activation of 伪-amino C-H bonds by B(C₆F₅)₃, which likely generates a “frustrated” acid/base complex in the presence of large N-alkylamines. The transformation requires no external oxidant and releases hydrosilane as a byproduct. The utility of this method is demonstrated in the late-stage functionalization of bioactive mols. such as citalopram, atomoxetine, and fluoxetine. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Quality Control of 1,2,2,6,6-Pentamethylpiperidine).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Quality Control of 1,2,2,6,6-Pentamethylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cobaltate anion couples terminal dienes with trifluoroacetic anhydride: a direct fluoroacylation of 1,3-dienes was written by Kohn, Benjamin L.;Rovis, Tomislav. And the article was included in Chemical Science in 2014.Application of 79-55-0 This article mentions the following:

Cobalt-mediated fluoroacylation of 1,3-dienes using perfluorinated anhydrides such as TFAA was described. The reaction proceeded through a fluoroacylcobalt reagent which formed in-situ. Perfluoroacylation of 1,3 dienes was also performed to attain longer chain perfluorinated ketones. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Application of 79-55-0).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application of 79-55-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Regio- and Stereoselective Synthesis of 1,2-cis-Glycosides by Anomeric O-Alkylation with Organoboron Catalysis was written by Izumi, Sanae;Kobayashi, Yusuke;Takemoto, Yoshiji. And the article was included in Organic Letters in 2019.Formula: C10H21N This article mentions the following:

Regio- and stereoselective synthesis of 1,2-cis-glycosides has been achieved by catalytic anomeric O-alkylation using organoboron compounds Modulating steric and electronic factors of both catalysts and substrates enables activation of the axially oriented anomeric oxygens of glucose-derived dialkoxyborates. The mild reaction conditions allow broad functional-group tolerance. This approach can be applied to the efficient sequential synthesis of oligosaccharides. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Formula: C10H21N).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) 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. 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.Formula: C10H21N

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cobaltate anion couples terminal dienes with trifluoroacetic anhydride: a direct fluoroacylation of 1,3-dienes was written by Kohn, Benjamin L.;Rovis, Tomislav. And the article was included in Chemical Science in 2014.Application of 79-55-0 This article mentions the following:

Cobalt-mediated fluoroacylation of 1,3-dienes using perfluorinated anhydrides such as TFAA was described. The reaction proceeded through a fluoroacylcobalt reagent which formed in-situ. Perfluoroacylation of 1,3 dienes was also performed to attain longer chain perfluorinated ketones. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Application of 79-55-0).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application of 79-55-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Regio- and Stereoselective Synthesis of 1,2-cis-Glycosides by Anomeric O-Alkylation with Organoboron Catalysis was written by Izumi, Sanae;Kobayashi, Yusuke;Takemoto, Yoshiji. And the article was included in Organic Letters in 2019.Formula: C10H21N This article mentions the following:

Regio- and stereoselective synthesis of 1,2-cis-glycosides has been achieved by catalytic anomeric O-alkylation using organoboron compounds Modulating steric and electronic factors of both catalysts and substrates enables activation of the axially oriented anomeric oxygens of glucose-derived dialkoxyborates. The mild reaction conditions allow broad functional-group tolerance. This approach can be applied to the efficient sequential synthesis of oligosaccharides. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Formula: C10H21N).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) 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. 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.Formula: C10H21N

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ring-Opening Polymerization with Lewis Pairs and Subsequent Nucleophilic Substitution: A Promising Strategy to Well-Defined Polyethylene-like Polyesters without Transesterification was written by Wang, Bin;Pan, Li;Ma, Zhe;Li, Yuesheng. And the article was included in Macromolecules (Washington, DC, United States) in 2018.Synthetic Route of C10H21N This article mentions the following:

Ring-opening polymerization (ROP) of ω-pentadecalactone (PDL) catalyzed by Lewis pairs was thoroughly explored, and a novel approach to well-defined aliphatic long chain polyester with high mol. weight (MW) was developed in the present work. The Zn(C₆F₅)₂/1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) Lewis pair was proved to be a promising catalytic system for ROP of PDL, producing cyclic PPDL with high MW (M_w > 100 kg/mol) and relatively low polydispersity index (M_w/M_n = 1.6-1.9). Strikingly, no transesterification occurred in the ROP of PDL by Zn(C₆F₅)₂/DBU. The cyclic topol. of the polyester could be switched to linear structure in the presence of alc. The feeding mode and the structure of alc. significantly influence the ROP. Compared with mixing alc. with Zn(C₆F₅)₂/DBU at first, adding Ph₂CHOH with low nucleophilicity after full monomer conversion could afford linear PPDL without transesterification. It was noted that random chain scission or chain extension was not detected after adding Ph₂CHOH. Well-defined block copolymer containing polyethylene-like segment can be easily prepared by sequential addition of PDL and lactide (LA) or caprolactone (CL). Cyclic block copolyesters c-poly(PDL-b-CL) and c-poly(PDL-b-LA) were obtained in the absence of alc. The blocky structures can be maintained even when prolonging reaction time after full monomer conversion. Similarly, introducing Ph₂CHOH before quenching the polymerization led to well-defined linear block copolyesters l-poly(PDL-b-CL) and l-poly(PDL-b-LA). In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Synthetic Route of C10H21N).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. 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.Synthetic Route of C10H21N

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem