Category: 10472-24-9

On December 28, 2020, Yu, Bao; Perfetto, Anna; Allievi, Luca; Dhambri, Sabrina; Rager, Marie-Noelle; Selkti, Mohamed; Ciofini, Ilaria; Lannou, Marie-Isabelle; Sorin, Geoffroy published an article.Computed Properties of 10472-24-9 The title of the article was Silver(I) Oxide-/DBU-Promoted Synthesis of Dihydrofuran Units through Allenyl Silver Formation. And the article contained the following:

Herein, a formal [3+2] cyclization mediated by silver(I) oxide and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) was described. Through a broad variety of carbonyl compounds, this system can promote cyclization reactions with high yield (up to 85%) and diastereoselectivity (up to 95:5) for a straightforward access to complex and congested dihydrofuran derivatives in one step under mild conditions. Based on DFT studies, the proposed mechanism would involve an allenyl silver intermediate. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Computed Properties of 10472-24-9

The Article related to polycyclic dihydrofuran preparation, keto ester silver catalyst diastereoselective heterocyclization, allenyl silver, dihydrofuran, intramolecular cyclization, isomerization and other aspects.Computed Properties of 10472-24-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 1, 2019, Wang, Shuai; Li, Zhong-Rui; Suo, Feng-Zhi; Yuan, Xiao-Han; Yu, Bin; Liu, Hong-Min published an article.Recommanded Product: 10472-24-9 The title of the article was Synthesis, structure-activity relationship studies and biological characterization of new [1,2,4]triazolo[1,5-a]pyrimidine-based LSD1/KDM1A inhibitors. And the article contained the following:

The design, synthesis and biochem. characterization of [1,2,4]triazolo[1,5-a]pyrimidine derivatives I [R1 = H, [(2-bromophenyl)methyl]sulfanyl, prop-2-en-1-ylsulfanyl, [(1H-1,3-benzodiazol-2-ylmethyl)sulfanyl], etc.; R2 = H, Me, (CH2)4CH3; R3 = Me, Et, C6H5; R2, R3 = -(CH2)3-; R4 = H, C6H5, [4-(4-methylpiperazin-1-yl)phenyl], etc.] as new LSD1 inhibitors have been reported. Of these compounds, compound I [R1 = (1H-1,3-benzodiazol-2-ylsulfanyl)methyl; R2 = H; R3 = Me; R4 = [4-(4-methylpiperazin-1-yl)phenyl]] (II) inhibited LSD1 in a reversible manner (IC50 = 1.72 μM) and showed selectivity to LSD1 over MAO-A/B. Besides, compound II displayed FAD-competitive binding to LSD1. Interestingly, compound II did not inhibit horseradish peroxidase (HRP) and quench H2O2, thus excluding the possibility that LSD1 inhibition by compound II was due to the HRP inhibition and consumption of H2O2. In LSD1 overexpressed A549 cells, compound II concentration-dependently induced accumulation of H3K4me1/me2 and H3K9me2 and showed cellular target engagement to LSD1. Addnl., compound II significantly inhibited migration of A549 cells in a concentration-dependent manner, further western blot anal. showed that compound II increased expression levels of epithelial cell markers E-Cadherin and Claudin-1, down-regulated mesenchymal cell marker N-Cadherin and the upstream transcription factors Snail and Slug. Docking studies were also performed to rationalize the potency of compound II toward LSD1. To conclude, the [1,2,4]triazolo[1,5-a]pyrimidine I could serve as a promising scaffold for the development of new LSD1 inhibitors. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Recommanded Product: 10472-24-9

The Article related to triazolopyrimidine preparation sar lsd1 kdm1a inhibitor anticancer activity, antiproliferative activity, lsd1 inhibitors, migration inhibition, [1,2,4]triazolo[1,5-a]pyrimidines and other aspects.Recommanded Product: 10472-24-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 30, 2021, Zhou, Shiyang; Zou, Huiying; Huang, Gangliang; Chen, Guangying; Zhou, Xueming; Huang, Shuheng published an article.Recommanded Product: Methyl 2-cyclopentanonecarboxylate The title of the article was Design, synthesis and anti-rheumatoid arthritis evaluation of double-ring conjugated enones. And the article contained the following:

Four series of double-ring conjugated enones were designed, synthesized and studied for the inhibition of synovial cell activity through the modification of Dysodensiol K core structure, double-ring, double-bond and double-carbonyl groups. For the in vitro synovial cell assay of rats, compound I and II exhibited good inhibitory activities, with IC50 values of 2.71 ± 0.18 and 2.68 ± 0.16μM, resp. At the same time, the LDH release and LD50 test results revealed that the target compounds had low cytotoxicity and acute toxicity. For the in vivo CIA model test through oral administration, compounds I and II exhibited a similar effect to pos. control group methotrexate. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Recommanded Product: Methyl 2-cyclopentanonecarboxylate

The Article related to dysodensiol k analog preparation antirheumatoid arthritis, synovial cell activity inhibitor dysodensiol k analog, conjugated enones, design, modification, synovial cell, synthesis and other aspects.Recommanded Product: Methyl 2-cyclopentanonecarboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On October 15, 2019, Lei, Hongrui; Jia, Fang; Cao, Meng; Wang, Jie; Guo, Ming; Zhu, Minglin; Zuo, Daiying; Zhai, Xin published an article.Synthetic Route of 10472-24-9 The title of the article was An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects. And the article contained the following:

The pyrimidine-2,4-diamine analogs exerted excellent activities in down-regulation of ALK phosphorylation. However, the prevalent drug-resistant site-mutation has gradually prevented the agents from being widely used. Herein, we conducted an exploration of high affinity moiety that bound to the solvent-front region (G1202R located) within the ATP binding site of ALK leading to the synthesis of thirty-five pyrimidine-2,4-diamine derivatives Among these compounds, urea group was extensively derivatized which finally resulted in the identification of the ‘semi-free urea’ compound 39. All compounds were assayed cytotoxicity and enzymic activities and 39 turned out to be the most potent one with IC50 values of 2.1, 0.91, 4.3 and 0.73 nM towards ALKwt, ALKL1196M, ALKG1202R and ROS1, resp. The performances of 39 on ALK- & ROS1-dependent cell lines were in good accordance with enzymic activities with IC50 values below 0.06μM. Besides, 39 induced cell apoptosis in a dose-dependent manner in H2228 cells. Finally, the binding models of 39 with ALKwt, ROS1, ALKL1196M and ALKG1202R were ideally established which further clearly elucidated their mode of action within the active site. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Synthetic Route of 10472-24-9

The Article related to pyrimidine diamine derivative preparation alk ros1 inhibitor resistant cancer, 4-diamine, alk & ros1 inhibitors, apoptosis-inducing, mutation-combating, pyrimidine-2, solvent front and other aspects.Synthetic Route of 10472-24-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On June 5, 2020, Jang, Sumin; Kim, Hyunwoo published an article.Recommanded Product: Methyl 2-cyclopentanonecarboxylate The title of the article was Chiral 1H NMR Analysis of Carbonyl Compounds Enabled by Cationic Cobalt Complex. And the article contained the following:

The authors report a newly prepared cationic cobalt(III) complex as a general and efficient chiral solvating agent that discriminates carbonyl compounds including esters, amides, ketones, and aldehydes. This cobalt(III) complex was further utilized to directly analyze both the conversion and the enantiomeric excess at once in the asym. fluorination. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Recommanded Product: Methyl 2-cyclopentanonecarboxylate

The Article related to chiral proton nmr analysis carbonyl compound cationic cobalt complex, crystal mol structure cobalt diphenylethylenediamine cyclohexanediamine dihydroxyphenylmethyl derivative complex and other aspects.Recommanded Product: Methyl 2-cyclopentanonecarboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Nassar, Youssef; Piva, Olivier published an article in 2021, the title of the article was Photoredox-catalyzed hydroxymethylation of β-ketoesters: application to the synthesis of [3.3.3] propellane lactones.Application of 10472-24-9 And the article contains the following content:

Photoredox-catalyzed hydroxymethylation of β-ketoesters substituted by an allyl subunit on the α-position afforded directly the corresponding bicyclic lactones possessing both a hydroxy group and an unsaturation A subsequent regioselective iodoetherification led to the formation of original [3.3.3] propellane structures. Substitution of the iodine atom by various nucleophiles afforded highly functionnalized structures including triazolomethyl derivatives The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Application of 10472-24-9

The Article related to ketoester diastereoselective hydroxymethylation, bicyclic lactone preparation iodoetherification, propellane lactone preparation, triazolomethyl propellane lactone preparation click chem and other aspects.Application of 10472-24-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On March 15, 2019, Li, Zhong-Rui; Wang, Shuai; Yang, Linlin; Yuan, Xiao-Han; Suo, Feng-Zhi; Yu, Bin; Liu, Hong-Min published an article.Safety of Methyl 2-cyclopentanonecarboxylate The title of the article was Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors. And the article contained the following:

Phenelzine was first employed to design new aryl hydrazine-based LSD1 inhibitors based on the experience-based discovery (EBD) strategy. Among these compounds, D8 potently inhibited LSD1 (IC50 = 882.30 nM) in a reversible manner. Compound D8 was selective to LSD1 over MAO-A/B and showed H3K4me2 competitive binding to LSD1. The interaction between H3K4me2 and LSD1 was also confirmed by the Co-IP assay. In LSD1 overexpressed A549 cells, compound D8 dose-dependently induced accumulation of LSD1 substrates H3K4me1/2 and H3K9me1/2, showed cellular target engagement to LSD1 and significantly inhibited cell migration of A549 cells. Docking studies suggested that compound D8 occupied the peptide binding region and therefore blocked the access of the peptide substrate to the FAD, finally leading to the demethylase activity inhibition of LSD1. The findings indicate that aryl hydrazines are new scaffolds for the design of LSD1 inhibitors, the identification of D8 provides further evidence for our previously proposed general principle that fused heterocycles with an amine group are potentially active toward LSD1 by competitive binding to LSD1 with H3 peptide substrates. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Safety of Methyl 2-cyclopentanonecarboxylate

The Article related to lsd1 inhibitor experience discovery aryl hydrazine scaffolds, aryl hydrazines, epigenetic regulation, experience-based discovery, lsd1 inhibitors, [1, 2, 4] triazolo[1, 5- a] pyrimidine and other aspects.Safety of Methyl 2-cyclopentanonecarboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 30, 2020, Trofymchuk, Serhii A.; Kliukovskyi, Denys V.; Semenov, Sergey V.; Khairulin, Andrii R.; Shevchenko, Valerii O.; Bugera, Maksym Y.; Tarasenko, Karen V.; Volochnyuk, Dmitriy M.; Ryabukhin, Sergey V. published an article.Electric Literature of 10472-24-9 The title of the article was Semi-Industrial Fluorination of β-Keto Esters with SF4 : Safety vs Efficacy. And the article contained the following:

The possibility of deoxofluorination of β-keto esters using SF4 was investigated. The scope and limitation of the reaction were determined The efficient method for the synthesis of β,β-difluorocarboxylic acids was elaborated based on the reaction. The set of mentioned acids, being the perspective building blocks for medicinal chem., were synthesized on multigram scale. The safety of SF4 use was discussed. The described method does not improve upon the safety of using SF4, but practical recommendations for working with the reagent were proposed. Despite the hazards of using toxic SF4, a significant increase of efficacy in the synthesis of medicinal-chem.-relevant building blocks, based on the reaction, in comparison with earlier described approaches was shown. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Electric Literature of 10472-24-9

The Article related to safety usage sulfur tetrafluoride deoxofluorination, ketoester sulfur tetrafluoride deoxofluorination, fluoroalkyl ester preparation hydrolysis, fluoro alkyl carboxylic acid preparation and other aspects.Electric Literature of 10472-24-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On July 31, 2021, Chhanda, Sadia Afrin; Itsuno, Shinichi published an article.Category: esters-buliding-blocks The title of the article was Synthesis of cinchona squaramide polymers by Yamamoto coupling polymerization and their application in asymmetric Michael reaction. And the article contained the following:

Yamamoto coupling polymerization was used for the synthesis of polymeric chiral organocatalysts. Cinchona squaramide derivatives with dibromophenyl moiety were polymerized under the Yamamoto coupling conditions to afford the corresponding chiral polymers in good yields. Using this technique, novel cinchona alkaloid polymers containing the squaramide moiety were designed and successfully synthesized. In addition to the homopolymerization of cinchona squaramide monomers with a dibromophenyl group, achiral comonomers such as dibromobenzene were copolymerized with the cinchona monomers to yield chiral co-polymers. These chiral polymers were successfully utilized as polymeric catalysts in asym. Michael addition reactions. Good to excellent enantioselectivities were observed for different types of asym. Michael reactions. Using the chiral homopolymer catalyst I, almost perfect diastereoselectivity (>100:1) with 99% ee were obtained for the reaction between Me 2-oxocyclopentanecarboxylate and trans-β-nitrostyrene. The polymer catalysts developed in this study have robust structures and can be reused several times without a loss in their catalytic activities. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Category: esters-buliding-blocks

The Article related to cinchona squaramide polymer catalyst preparation yamamoto coupling, styrene anthrone copolymer catalyst enantioselective michael addition reaction, phenylethyl anthracenone preparation and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Berger, Anna Lucia; Donabauer, Karsten; Koenig, Burkhard published an article in 2019, the title of the article was Photocatalytic carbanion generation from C-H bonds – reductant free Barbier/Grignard-type reactions.Formula: C7H10O3 And the article contains the following content:

A redox-neutral method for the generation of carbanions from benzylic C-H bonds in a photocatalytic Grignard-type reaction was reported. The combination of photo- and hydrogen atom transfer (HAT) catalysis enabled the abstraction of a benzylic hydrogen atom, generating a radical intermediate. This radical was reduced in situ by the organic photocatalyst to a carbanion, which was able to react with electrophiles such as aldehydes or ketones, yielding homobenzylic secondary and tertiary alcs. ArCR1R2C(OH)R3R4 [R1 = R2 = H, Me, R1 = H, R2 = Me; R3 = R4 = Me, Et, n-Bu, R3 = H, Me, R4 = Me, Et, i-Pr, etc; Ar = 2-thienyl, Ph, 4-MeOC6H4, etc.]. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Formula: C7H10O3

The Article related to organo photocatalyst preparation, tertiary alc preparation, ketone alkyl benzene barbier grignard reaction, secondary alc preparation, aldehyde alkyl benzene barbier grignard reaction and other aspects.Formula: C7H10O3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics