Tag: 100-200

Goma’a, Hebat-Allah M.; Ghaly, Mariam A.; Abou-zeid, Laila A.; Badria, Farid A.; Shehata, Ihsan A.; El-Kerdawy, Mohamed M. published an article in 2019, the title of the article was Synthesis, Biological Evaluation and In Silico Studies of 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives as Antiherpetic Agents.Recommanded Product: 3-Acetyldihydrofuran-2(3H)-one And the article contains the following content:

Two isosteric series of 1,2,4-triazole and 1,3,4-thiadiazole derivatives were synthesized and evaluated for their antiviral activity against herpes simplex virus type 1, HSV-1, using acyclovir (ACV) as a reference drug. In addition, mol. docking into the active site of HSV-1 thymidine kinase was performed to interpret the data obtained from biol. testing, and all compounds were subjected to an in-silico screening of their physicochem. properties to estimate their drug-likeness and safety. The results revealed that triazolopyrimidine derivative I was able to reduce the viral plaques by 50% at a dose of 80 μM, but interestingly, retained high selectivity compared to ACV (>200 μM vs. 80 μM). The best effective and safe compound in this study, triazolopyrimidine derivative I, was further tested for its combined effects with ACV on the anti-HSV-1 activity in the plaque reduction assay. This compound proved to improve the selectivity of ACV and reduce its ED that produced 100% inhibition of viral plaques. The compound I was suggested to be a promising candidate for further development as an antiherpetic agent. Mol. docking into the active site of HSV-1 thymidine kinase emphasized the superior interaction of the compound I. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Recommanded Product: 3-Acetyldihydrofuran-2(3H)-one

The Article related to triazole thiadiazole preparation antiherpetic activity docking cytotoxicity, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 3-Acetyldihydrofuran-2(3H)-one

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

On August 19, 2010, Bollu, Venkataiah; Boren, Brant Clayton; Dalgard, Jackline Eve; Flatt, Brenton T.; Haq, Nadia; Hudson, Sarah; Mohan, Raju; Morrissey, Michael; Pratt, Benjamin; Wang, Tie-Lin published a patent.Electric Literature of 86239-00-1 The title of the patent was Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity and their preparation. And the patent contained the following:

The present invention comprises TGR5 agonists of structural formula I, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated. Compounds of formula I wherein X is N, CPh, CR4, etc.; R1 is Ph, C5-6 cycloalkyl, CH2phenyl, etc.; R2 is [CR2]pY[CR2]q-R6; p and q are independently 0 and 1; each R is independently H, C1-3 alkyl, halo, OH and CH2OH; Y is a bond, S, SO2, CHOH, O, etc.; R6 is C6-10 aryl, NH-Ph, cycloalkyl, etc.; R2 is R4 is H, C1-3 alkyl, and halo; R5 is CH2phenyl, CH2naphthalenyl, CH2-heteroaryl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by S-alkylation of 5-(2-(3,4-dimethoxyphenyl)propan-2-yl)-1-(4-fluorophenyl)-1H-imidazole-2(3H)-thine with 2-chloro-4-fluorobenzyl bromide. All the invention compounds were evaluated for their TGR5 agonistic activity (some data given). The experimental process involved the reaction of Ethyl 3-fluoro-4-methylbenzoate(cas: 86239-00-1).Electric Literature of 86239-00-1

The Article related to imidazole triazole preparation tgr5 agonist treatment diabetes obesity, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 86239-00-1

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

On November 30, 2014, Ding, Chao; Wei, Weili; Sun, Hanjun; Ding, Jinhua; Ren, Jinsong; Qu, Xiaogang published an article.Electric Literature of 3976-69-0 The title of the article was Reduced graphene oxide supported chiral Ni particles as magnetically reusable and enantioselective catalyst for asymmetric hydrogenation. And the article contained the following:

A reduced graphene oxide (rGO) supported chiral-modified Ni catalyst was synthesized, characterized and employed for asym. hydrogenation. The prepared hybrid catalyst could produce each enantiomer with D- or L-tartaric acid as chiral modifier and exhibited a high TOF (20160 h-1) and enantioselectivity (enantiomeric excess, 98.5%) for asym. hydrogenation of Me acetoacetate. The high catalytic activity and enantioselectivity were mainly attributed to the unique properties of the support rGO, as it had a large sp. surface area to sustain and stabilize Ni particles and its high charge carrier mobility could enable the readily transfer of electrons in the reaction process. Besides, the catalyst could also gain an enhanced reactant sorption with the support of rGO, thus achieved a greatly catalysis enhancement. The ferromagnetism of Ni made the catalyst easier for separation and reuse. The catalytic and recycling performance of the prepared chiral Ni catalyst demonstrated that rGO was indeed a promising support to improve activity, enantioselectivity and durability of catalysts, and the prepared catalysts were promising reusable heterogeneous catalysts for asym. hydrogenation. The experimental process involved the reaction of (R)-Methyl 3-hydroxybutanoate(cas: 3976-69-0).Electric Literature of 3976-69-0

The Article related to reduced graphene oxide supported nickel magnetically reusable enantioselective catalyst, asym hydrogenation enantioselective reduced graphene oxide supported nickel, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Electric Literature of 3976-69-0

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

On September 24, 2009, Foulon, Loiec; Goullieux, Laurent; Pouzet,brigitte; Serradeil-Le Gal, Claudine; Valette, Gerard published a patent.Recommanded Product: 872046-08-7 The title of the patent was Preparation of 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives as selective V1a arginine vasopressin receptor ligands and in some cases as V1b ligands as well. And the patent contained the following:

The invention is related to the preparation of 3-aminoalkylindolin-2-one derivatives I [X = C1-5 alkylene optionally substituted at ≥1 C atoms by 1 F or by a C1-3 alkyl; R1 = NR8R9, (un)substituted piperidin-4-yl, piperidin-3-yl; R8, R9 = independently H, alkyl; or NR8R9 = heterocyclyl selected from azetidin-4-yl, pyrrolidin-4-yl, morpholin-4-yl, piperazin-4-yl, etc., the C atoms being optionally substituted by ≥1 F atoms; R2 = halo, Alk, OAlk; Alk = = alkyl optionally substituted by ≥1 F atoms; R3 = OMe; R4, R7 = independently H, halo, OH, Alk, OAlk; R5 = H, CO2Alk, CH2OH, R4; R6 = H, OH, Alk, OAlk, cycloalkyloxy, NHCONH2 and derivatives; or R7 is in the 3-position of the Ph group and together with R6 they represent a CH2CH2CH2 radical] their acid addition salts and their hydrates or solvates, having a strong affinity and high selectivity for human V1a arginine vasopressin receptors and in some cases also a strong affinity for V1b receptors. Thus, a multi-step synthesis from 1-chloro-5-fluoro-2-methoxy-4-nitrobenzene and Me 2-(2-fluorophenyl)acetate was given for indolinone (+)-II·×HCl. In an in vitro assay, II bound selectively to human V1a receptor with IC50 = 2.4 nM compared to human V1b, human V2 vasopressin receptors and human oxytocin receptor (Ic50 = >1000 nM, 450 nM and 390 nM, resp.). The V1a antagonistic activity of II was determined in vitro in a FLIPR test measuring the intracellular calcium in cells expressing the human V1a receptors. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Recommanded Product: 872046-08-7

The Article related to indolinone aminoalkyl preparation selective v2 vasopressin antagonist, vasopressin v2 receptor ligand aminoalkyldihydrohindolone preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 872046-08-7

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

Kang, Houng; Jemison, Adriana L.; Nigro, Erin; Kozlowski, Marisa C. published an article in 2019, the title of the article was Oxidative Coupling of 3-Oxindoles with Indoles and Arenes.Related Products of 85-91-6 And the article contains the following content:

A highly efficient method for the oxidative coupling of 2-substituted 3-oxindoles with aromatic compounds to form 2,2-disubstituted indolin-3-ones with broad scope is described. This work utilized oxygen as the terminal oxidant and a base-metal catalyst under mild conditions instead of toxic/precious-metal reagents and higher-mol.-weight oxidants. Quaternary structures were produced in modest-to-excellent yields (up to 96 %) without prefunctionalization. The experimental process involved the reaction of Methyl N-Methylanthranilate(cas: 85-91-6).Related Products of 85-91-6

The Article related to disubstituted indolinone preparation oxidative coupling indole oxindole, catalysis, coinage metals, oxidative coupling, oxygen, sustainable, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Related Products of 85-91-6

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

On October 15, 2021, Wu, Yinrong; Wen, Kangmei; Chen, Jiewen; Shi, Jie; Yao, Xingang; Tang, Xiaodong published an article.Name: Methyl 2-cyclopentanonecarboxylate The title of the article was Copper-Mediated Decarboxylative Coupling between Arylacetic Acids and 1,3-Dicarbonyl Compounds. And the article contained the following:

A copper-mediated decarboxylative coupling reaction between arylacetic acids and 1,3-dicarbonyl compounds was described for the synthesis of ((indolyl)methyl)-oxocycloalkyl-esters, e.g., I. Significantly, methanocycloocta[b]indoles II [R = COOEt, CONHEt, SO2Ph, etc.; R1 = H, 4-Cl, 5-Br, etc.] were also obtained by sequential intramol. dehydrocyclization process in some cases. This protocol featured a broad substrate scope, simple operations, and good yields. Moreover, the products exhibited potent antiproliferative activity against the human cancer cell lines by a MTT assay. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Name: Methyl 2-cyclopentanonecarboxylate

The Article related to indolyl methyl oxocycloalkyl ester preparation antitumor, arylacetic acid dicarbonyl compound decarboxylative coupling copper mediated, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Name: Methyl 2-cyclopentanonecarboxylate

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

On March 5, 2009, Xia, Ji-Bao; You, Shu-Li published an article.Application of 93476-46-1 The title of the article was Synthesis of 3-Haloindolizines by Copper(II) Halide Mediated Direct Functionalization of Indolizines. And the article contained the following:

3-Haloindolizines were synthesized via Cu(II) halide mediated halogenation of indolizines. This C-H direct functionalization process occurred under mild conditions giving 3-haloindolizines in moderate to excellent yields, and the products obtained were tested under the Suzuki-Miyaura reaction providing 3-arylindolizines in high yields. The experimental process involved the reaction of Ethyl indolizine-1-carboxylate(cas: 93476-46-1).Application of 93476-46-1

The Article related to regioselective preparation haloindolizine cupric halide mediated halogenation indolizine, suzuki miyaura reaction haloindolizine, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 93476-46-1

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

Sako, Makoto; Higashida, Keigo; Kamble, Ganesh Tatya; Kaut, Kevin; Kumar, Ankit; Hirose, Yuka; Zhou, Da-Yang; Suzuki, Takeyuki; Rueping, Magnus; Maegawa, Tomohiro; Takizawa, Shinobu; Sasai, Hiroaki published an article in 2021, the title of the article was Chemo- and enantioselective hetero-coupling of hydroxycarbazoles catalyzed by a chiral vanadium(V) complex.Safety of Methyl 2-cyclopentanonecarboxylate And the article contains the following content:

The catalytic enantioselective oxidative hetero-coupling of arenols using a chiral vanadium(V) complex has been developed. The coupling of hydroxycarbazole derivatives with various arenols provided axially chiral biarenols with high chemo-, regio-, and enantioselectivities. The reaction took place under mild conditions and exhibited satisfactory functional group tolerance. Aerobic oxidative hetero-coupling with β-ketoesters also proceeded with high chemo- and stereoselectivities under slightly modified reaction conditions. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Safety of Methyl 2-cyclopentanonecarboxylate

The Article related to biarenol preparation enantioselective chemoselective regioselective, hydroxycarbazole arenol oxidative hetero coupling vanadium, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Safety of Methyl 2-cyclopentanonecarboxylate

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

Wang, Chunjie; Jia, Huali; Li, Zhiwei; Zhang, Hui; Zhao, Baoli published an article in 2016, the title of the article was Palladium-catalyzed C-3 desulfitative arylation of indolizines with sodium arylsulfinates and arylsulfonyl hydrazides.HPLC of Formula: 93476-46-1 And the article contains the following content:

Derivatized indolizines I (R = 4-CH3OC6H4, 4-FC6H4, 3-BrC6H4, 2-naphthyl, etc.) were efficiently prepared by direct C-3 arylation of indolizines using sodium arylsulfinates and arylsulfonyl hydrazides. Pd-catalyzed desulfitative C-3 arylation with sodium arylsulfinates was achieved with the assistance of peroxides, and the catalytic efficiency was promoted by N-containing ligands. Arylsulfonyl hydrazides were also successfully applied in Pd-catalyzed desulfitative C-3 arylation with indolizines, and the side homocoupling reactions can be restrained in the component solvent under milder conditions. Various derivatives were synthesized in good yields by both methods, offering expedient protocols for the synthesis of C-3 functionalized indolizine mols. The experimental process involved the reaction of Ethyl indolizine-1-carboxylate(cas: 93476-46-1).HPLC of Formula: 93476-46-1

The Article related to indolizine preparation, sodium arylsulfinate arylsulfonyl hydrazide indolizine desulfitative arylation palladium catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.HPLC of Formula: 93476-46-1

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

On March 6, 2015, Hu, Huayou; Li, Guodong; Hu, Weiming; Liu, Yun; Wang, Xiang; Kan, Yuhe; Ji, Min published an article.Formula: C11H11NO2 The title of the article was Synthesis of Pyrrolo[2,1,5-cd]indolizines through Dehydrogenative Heck Annelation of Indolizines with Diaryl Acetylenes Using Dioxygen as an Oxidant. And the article contained the following:

A dehydrogenative Heck annelation reaction of indolizine with diaryl acetylene via dual C-H bond cleavage was developed. Oxygen gas was employed as a clean oxidant in this catalysis under base-free conditions. Diarylpyrrolo[2,1,5-cd]indolizines were synthesized with high atom economy. In addition, kinetic isotope experiments provided evidence for C-H bond metalation of the 5-position of the indolizine as the rate-limiting step. The experimental process involved the reaction of Ethyl indolizine-1-carboxylate(cas: 93476-46-1).Formula: C11H11NO2

The Article related to dehydrogenative heck annelation indolizine diaryl alkyne palladium catalyst, pyrroloindolizine diaryl preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C11H11NO2

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