Category: 517-23-7

On November 15, 2021, Said, Mona F.; Georgey, Hanan H.; Mohammed, Eman R. published an article.Synthetic Route of 517-23-7 The title of the article was Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. And the article contained the following:

Addressing the global need for the development of safe and potent NSAIDs, new series of oxadiazolo and thiadiazolo fused pyrmidinones were synthesized and initially tested for their analgesic activity. All tested compounds showed promising analgesic activity compared with the reference standard indomethacin. Moreover, anti-inflammatory activity evaluation, ulcerogenic liability, and in vitro COX-1, COX-2 enzyme inhibition assays were also performed for the most active derivatives The methoxyphenyl piperazinyl derivative I showed analgesic activity surpassing indomethacin with protection of 100%, and 83%; resp. Also I showed good anti-inflammatory activity with relatively lower ulcer index compared with other tested compounds, and potent COX-1 and COX-2 inhibitory activity with IC50 = 0.140, 0.007μm, resp., and with a selectivity index of 20.00 which was better than the reference standards and the other tested congeners. Addnl., three compounds revealed moderate selectivity (SI = 3.53, 3.70 and 5.87, resp.). Moreover, in silico physicochem. parameters revealed that the new fused pyrimidinones demonstrated promising pharmacokinetic properties. Furthermore, computational studies in form of 2D-quant. structure-activity relationship (2D-QSAR) and 3D-pharmacophore confirmed the potential analgesic properties of the new target compounds The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Synthetic Route of 517-23-7

The Article related to fused pyrimidinone preparation antiinflammatory physicochem analgesic pharmacophore pharmacokinetic, analgesic, anti-inflammatory, fused pyrimidinones, pharmacophore, qsar study and other aspects.Synthetic Route of 517-23-7

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

On April 13, 2022, Xu, Yan-Li; Wang, Yu-Xia; Wen, Gen-Fa; Da, Chao-Shan published an article.Synthetic Route of 517-23-7 The title of the article was Organocatalytic enantioselective electrophilic amination of benzoyl butyrolactones. And the article contained the following:

Organocatalytic electrophilic amination of benzoyl butyrolactones with azodicarboxylates was demonstrated to highly efficiently prepare quaternary carbon stereocenter-bearing α-amino-γ-butyrolactones I [R = Me, Ph, OBn, etc.], key framework in numerous bioactive compounds The squaramide catalyst II realized the highest yield (99%) and enantioselectivity (93%). The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Synthetic Route of 517-23-7

The Article related to squaramide catalyst preparation, alpha amino gamma butyrolactone enantioselective preparation, benzoyl butyrolactone azodicarboxylate squaramide catalyst electrophilic amination and other aspects.Synthetic Route of 517-23-7

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

On March 31, 2019, Chen, Kai; Huang, Xiongyi; Zhang, Shuo-Qing; Zhou, Andrew Z.; Kan, S. B. Jennifer; Hong, Xin; Arnold, Frances H. published an article.SDS of cas: 517-23-7 The title of the article was Engineered Cytochrome c-Catalyzed Lactone-Carbene B-H Insertion. And the article contained the following:

Previous work has demonstrated that variants of a heme protein, Rhodothermus marinus cytochrome c(Rma cyt c), catalyze abiol. carbene boron-hydrogen (B-H) bond insertion with high efficiency and selectivity. Here authors investigated this carbon-boron bond-forming chem. with cyclic, lactone-based carbenes. Using directed evolution, they obtained a Rma cyt c variant BORLAC that shows high selectivity and efficiency for B-H insertion of 5- and 6-membered lactone carbenes (up to 24,500 total turnovers and 97.1:2.9 enantiomeric ratio). The enzyme shows low activity with a 7-membered lactone carbene. Computational studies revealed a highly twisted geometry of the 7-membered lactone carbene intermediate relative to 5- and 6-membered ones. Directed evolution of cytochrome c together with computational characterization of key iron-carbene intermediates has allowed us to expand the scope of enzymic carbene B-H insertion to produce new lactone-based organoborons. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).SDS of cas: 517-23-7

The Article related to cytochrome c catalyzed lactone carbene boron hydrogen insertion, mol structure calculation hemeprotein biocatalyst, biocatalyst, carbene, cytochrome c, directed evolution, lactones, organoboron and other aspects.SDS of cas: 517-23-7

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

Pisella, Guillaume; Gagnebin, Alec; Waser, Jerome published an article in 2020, the title of the article was Three-Component Reaction for the Synthesis of Highly Functionalized Propargyl Ethers.Formula: C6H8O3 And the article contains the following content:

Copper-catalyzed three-component reaction of diazo compounds, alcs. and ethynyl benziodoxole (EBX) reagents for the synthesis of propargyl ethers was reported. Extensive variations of the three partners of the reaction was possible, led to highly functionalized and structurally diverse products under mild conditions. Alkynylation of a copper ylide intermediate was postulated as key step for this transformation. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Formula: C6H8O3

The Article related to ethynyl benziodoxole alc diazo copper compound three component reaction, propargyl ether preparation, carbenes, copper catalysis, hypervalent iodine reagents, multi-component reactions (mcr), synthetic methods and other aspects.Formula: C6H8O3

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

On October 15, 2019, Liu, Ruiqi; Zhang, Zhuqing; Yang, Hong; Zhou, Kaixin; Geng, Meiyu; Zhou, Weicheng; Zhang, Mingming; Huang, Xun; Li, Yingxia published an article.Computed Properties of 517-23-7 The title of the article was Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. And the article contained the following:

In order to find potent p300 inhibitors with good drug-like properties, C646 was chosen as the lead compound and a series of new p300 inhibitors were designed based on the principle of bioisosterism and reasonable scaffold hopping and the structure-activity relationship was systematically explored. Ten of them were found to show comparable inhibitory activity as C646. The most potent pyrazolylidene compound, e.g., I (IC50 = 0.16 μM), showed better p300 inhibitory activity than C646 with improved drug-like properties. Western blotting experiment confirmed that pyrazolylidene compound, e.g., I could reduce the level of H3K27 acetylation more significantly than C646. Further cellular assay indicated that it could inhibit the proliferation of human breast ductal carcinoma cell T47D and human breast cancer cell MCF7 with the IC50 values of 5.08 μM and 22.54 μM, resp. Docking study of pyrazolylidene compound, e.g., I with p300 protein showed the possible reasons for its higher inhibition activity. Thus, pyrazolylidene compound, e.g., I might be with potential for development as a novel epigenetic agent targeting p300. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Computed Properties of 517-23-7

The Article related to phenylazolylidene phenylheteroarene preparation histone acetyltransferase p300 inhibition sar docking, c646, epigenetics, sensitive tumor cell proliferation, structure-activity relationship, p300 inhibitors and other aspects.Computed Properties of 517-23-7

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

On January 31, 2019, Bityukov, Oleg V.; Vil’, Vera A.; Lukashin, Nikita V.; Cherednichenko, Aleksandr G.; Nikishin, Gennady I.; Terent’ev, Alexander O. published an article.Product Details of 517-23-7 The title of the article was Solvent-free silica gel mediated decarboxylation of C-O coupling products of β-diketones and β-oxo esters with malonyl peroxides. And the article contained the following:

Silica gel was found to mediate decarboxylation of tetracarbonyl compounds with a free carboxylic group prepared from β-dicarbonyl compounds and malonyl peroxides to give I [R1 = Me; R2 = Me, CH2Ph, (CH2)2C(O)CH3, etc.; R1R2 = (CH2)3, (CH2)4, O(CH2)2; R3 = Me, OEt; R4 = CHEt2, CH(n-Bu)2, c-C4H7, c-C5H9]. Under solvent-free heterogeneous conditions silica gel effectively acts as a mediator of C-O coupling with further decarboxylation at 120 °C. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Product Details of 517-23-7

The Article related to acyloxy dicarbonyl compound preparation solventless, oxoester malonyl peroxide decarboxylation oxidative coupling silica gel catalyst, diketone malonyl peroxide decarboxylation oxidative coupling silica gel catalyst and other aspects.Product Details of 517-23-7

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

Saidalimu, Ibrayim; Yoshioka, Takuya; Liang, Yumeng; Tokunaga, Etsuko; Shibata, Norio published an article in 2018, the title of the article was The CF3-DAST-induced deacylative trifluoromethylthiolation of cyclic 1,3-diketones/lactams/lactones and its extension to deacylative pentafluorophenylthiolation.Electric Literature of 517-23-7 And the article contains the following content:

A trifluoromethyl analog of diethylaminosulfur trifluoride (CF3-DAST)-induced deacylative trifluoromethylthiolation of cyclic 1,3-diketones, lactams, and lactones that provide cyclic α-trifluoromethylthioketones, lactams, and lactones is reported. To the best of knowledge, this method represents the first example of the trifluoromethylthiolation of lactams. A corresponding deacylative pentafluorophenylthiolation using a pentafluorophenyl analog of diethylaminosulfur trifluoride (C6F5-DAST) was also attempted. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Electric Literature of 517-23-7

The Article related to trifluoromethylthio cyclic ketone lactam lactone preparation, cyclic diketone lactam lactone deacylative trifluoromethylthiolation diethylaminosulfur trifluoride, lactam cyclic diketone deacylative pentafluorophenylthiolation and other aspects.Electric Literature of 517-23-7

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

On January 31, 2018, Cao, Shi-Xuan; Wang, Jia-Xi; He, Zheng-Jie published an article.Category: esters-buliding-blocks The title of the article was Magnetic nanoparticles supported cinchona alkaloids for asymmetric Michael addition reaction of 1,3-dicarbonyls and maleimides. And the article contained the following:

Magnetic nanoparticles Fe3O4@SiO2 supported cinchona alkaloids (quinine and quinidine) were successfully synthesized as magnetically recoverable organocatalysts and characterized by FT-IR, XPS, SEM measurements, and elemental anal. Their catalytic activity and stereoselectivity were preliminarily evaluated in the asym. Michael addition reaction of 1,3-dicarbonyl compounds and maleimides to afford 3-(2-oxocyclopentyl)pyrrolidine-2,5-dione derivatives I [R = H, Me, Bn, etc.; R1 = C(O)Me, CO2Et, CO2Me], 3-[3-acetyl-2-oxo-tetrahydrofuran-3-yl]-1-benzyl-pyrrolidine-2,5-dione and ethyl-2-[1-benzyl-2,5-dioxo-pyrrolidin-3-yl]-3-oxo-butanoate. The supported quinine catalyst exhibited good catalytic efficiency and modest to high enantioselectivity. The magnetic recoverability and recyclability of the catalyst were also examined The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Category: esters-buliding-blocks

The Article related to silica coated magnetic nanoparticle supported cinchona alkaloid preparation, pyrrolidinedione preparation enantioselective diastereoselective, dione maleimide michael magnetic nanoparticle supported cinchona alkaloid catalyst and other aspects.Category: esters-buliding-blocks

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

On August 16, 2021, Liu, Xigong; Zhao, Changyin; Zhu, Rongxiu; Liu, Lei published an article.Application In Synthesis of 3-Acetyldihydrofuran-2(3H)-one The title of the article was Construction of Vicinal Quaternary Carbon Stereocenters Through Diastereo- and Enantioselective Oxidative 1,6-Conjugate Addition. And the article contained the following:

The asym. construction of vicinal quaternary carbon stereocenters with at least one moiety in acyclic systems is a formidable challenge. A solution involving diastereo- and enantioselective oxidative 1,6-conjugate addn was disclosed. The practical asym. cross-dehydrogenative coupling of 2,2-diarylacetonitriles and diverse α-substituted cyclic 1,3-dicarbonyls proceeds, for vicinal quaternary carbon stereocenters with one center in acyclic systems, in excellent yields and stereoselectivities. The generality of the approach was further demonstrated by the stereoselective creation of vicinal quaternary carbon stereocenters with both centers in acyclic systems using acyclic β-ketoesters as coupling partners. Computational studies elucidate the origins of both diastereo- and enantioselectivity. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Application In Synthesis of 3-Acetyldihydrofuran-2(3H)-one

The Article related to diarylacetonitrile keto ester copper catalyst enantioselective oxidative conjugate addition, diaryl cyanomethyl alkanone carboxylate preparation, 1,6-conjugate addition, asymmetric catalysis, cross-dehydrogenative coupling, synthetic methods, vicinal quaternary stereocenters and other aspects.Application In Synthesis of 3-Acetyldihydrofuran-2(3H)-one

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

On February 5, 2021, Liang, Ren-Xiao; Zhong, Chao; Liu, Zhi-Hong; Yang, Miao; Tang, Heng-Wei; Chen, Jian-Fei; Yang, Yun-Fang; Jia, Yi-Xia published an article.Product Details of 517-23-7 The title of the article was Enantioselective Arylation of Tetrasubstituted Enamines: Access to Enantioenriched Indolenine and 1H-Indole Derivatives. And the article contained the following:

Palladium-catalyzed intramol. enantioselective β-arylation of tetrasubstituted endocyclic and exocyclic enamines was developed. A range of optically active medium-ring fused indolenines or 3,3′-spiroindolenines were achieved in enantiomeric ratios up to 98:2 with Cs2CO3 or K3PO4 as the base in the presence of chiral PHOX ligands. The use of Ag3PO4 as a base led to enantioenriched 1H-indoles in good enantiomeric ratios (up to 89:11) with (S)-DIFLUORPHOS as a chiral ligand, which proceeded via a possible domino enamine-isomerization/β-arylation sequence. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Product Details of 517-23-7

The Article related to haloarylamino cycloalkenyl ester palladium catalyst enantioselective regioselective heteroarylation, cycloalkylpyrroloarene preparation, bromophenylaminomethylidene oxolanone palladium catalyst enantioselective regioselective heteroarylation, spirofuranindolone preparation and other aspects.Product Details of 517-23-7

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