Category: 5455-98-1

Borowiecki, Pawel; Zdun, Beata; Popow, Natalia; Wiklinska, Magdalena; Reiter, Tamara; Kroutil, Wolfgang published an article in 2022, the title of the article was Development of a novel chemoenzymatic route to enantiomerically enriched 尾-adrenolytic agents. A case study toward propranolol, alprenolol, pindolol, carazolol, moprolol, and metoprolol.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione And the article contains the following content:

Efficient chemoenzymic routes toward the synthesis of both enantiomers of adrenergic beta-blockers were accomplished by identifying a central chiral building block, which was first prepared using lipase-catalyzed kinetic resolution (KR, Amano PS-IM) as the asym. step at a five gram-scale (209 mM concentrate). The enantiopure (R)-chlorohydrin (>99% ee) subsequently obtained was used for the synthesis of a series of model (R)-(+)-beta-blockers (i.e., propranolol, alprenolol, pindolol, carazolol, moprolol, and metoprolol), which were produced with enantiomeric excess in the range of 96-99.9%. The pharmaceutically relevant (S)-counterpart, taking propranolol as a model, was synthesized in excellent enantiomeric purity (99% ee) via acetolysis of the resp. enantiomerically pure (R)-mesylate by using cesium acetate and a catalytic amount of 18-Crown-6, followed by acidic hydrolysis of the formed (S)-acetate. Alternatively, asym. reduction of a prochiral ketone, namely 2-(3-chloro-2-oxopropyl)-1H-isoindole-1,3(2H)-dione, was performed using lyophilized E. coli cells harboring overexpressed recombinant alc. dehydrogenase from Lactobacillus kefir (E. coli/Lk-ADH-Lica) giving the corresponding chlorohydrin with >99% ee. Setting the stereocenter early in the synthesis and performing a 4-step reaction sequence in a 鈥瞣ne-pot two-step鈥?procedure allowed the design of a 鈥瞫tep-economic鈥?route with a potential dramatic improvement in process efficiency. The synthetic method can serve for the preparation of a broad scope of enantiomerically enriched beta-blockers, the chem. structures of which rely on the common 伪-hydroxy-N-isopropylamine moiety, and in this sense, might be industrially attractive. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to adrenergic betha blocker one pot two step procedure, Placeholder for records without volume info and other aspects.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

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On November 30, 2015, Wang, Feng; Fan, Di; Qian, Jun; Zhang, Zhe; Zhu, Jianhua; Chen, Jian published an article.Synthetic Route of 5455-98-1 The title of the article was Preparation and Biodistribution of Technetium-99m-Labeled Bis- Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia. And the article contained the following:

Diagnosis of tumor hypoxia is an important aspect in determining the course of tumor therapy. In this study, we developed a novel imaging agent, 99mTcethylenedicysteine- bis-misonidazole (99mTc-EC-MISO), for diagnosing tumor hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labeling 99mTc in the second step. 99mTc-pertechnetate (99mTcO4 -) was reduced by tin chloride (SnCl2) for radiolabeling. The radiochem. purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on s.c. gliomal tumor-bearing mice. The tumor-to-muscle ratio in the 99mTc-EC-MISO group increased with time, up to 4.6 at 4 h after injection. SPECT/CT imaging confirmed that the tumors could be visualized clearly with 99mTc-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox center, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the tumor was observed The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Synthetic Route of 5455-98-1

The Article related to technetium 99m ecmiso spect ct biodistribution tumor hypoxia imaging, Placeholder for records without volume info and other aspects.Synthetic Route of 5455-98-1

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On April 30, 2011, Mugabe, Clement; Matsui, Yoshiyuki; So, Alan I.; Gleave, Martin E.; Heller, Markus; Zeisser-Labouebe, Magali; Heller, Lindsay; Chafeeva, Irina; Brooks, Donald E.; Burt, Helen M. published an article.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the article was In vitro and in vivo evaluation of intravesical docetaxel loaded hydrophobically derivatized hyperbranched polyglycerols in an orthotopic model of bladder cancer. And the article contained the following:

The objective of this study was to evaluate the tolerability, to establish a dosing regimen, and to evaluate the efficacy of intravesical docetaxel (DTX) formulations in a mouse model of bladder cancer. DTX in com. formulation (Taxotere, DTX in Tween 80) or loaded in hyperbranched polyglycerols (HPGs) was evaluated. The synthesis and characterization of HPGs with hydrophobic cores and derivatized with methoxy poly(ethylene glycol) in the shell and further functionalized with amine groups (HPG-C8/10-MePEG and HPG-C8/10-MePEG-NH2) is described. Intravesical DTX in either com. or HPGs formulations (up to 1.0 mg/mL) was instilled in mice with orthotopic bladder cancer xenografts and was well tolerated with no apparent signs of local or systemic toxicities. Furthermore, a single dose of intravesical DTX (0.5 mg/mL) loaded in HPGs was significantly more effective in reducing the tumor growth in an orthotopic model of bladder cancer than the com. formulation of Taxotere. In addition, DTX-loaded HPG-C8/10-MePEG-NH2 was found to be more effective at lower instillation dose than DTX (0.2 mg/mL)-loaded HPG-C8/10-MePEG. Overall, our data show promising antitumor efficacy and safety in a recently validated orthotopic model of bladder cancer. Further research is warranted to evaluate its safety and efficacy in early phase clin. trials in patients refractory to standard intravesical therapy. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to hyperbranched polyglycerol amino peg nanoparticle docetaxel bladder cancer, Pharmaceuticals: Pharmaceutics and other aspects.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

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On November 30, 2016, Guillon, Jean; Moreau, Stephane; Ronga, Luisa; Basmacyian, Louise; Cohen, Anita; Rubio, Sandra; Bentzinger, Guillaume; Savrimoutou, Solene; Azas, Nadine; Mullie, Catherine; Sonnet, Pascal published an article.HPLC of Formula: 5455-98-1 The title of the article was Design, Synthesis and Antimalarial Activity of Some New Aminoalcoholpyrrolo[1,2-a]quinoxaline Derivatives. And the article contained the following:

Following our search for antimalarial compounds, novel series of piperazinylalc. pyrrolo[ 1,2-a]quinoxaline derivatives 1-2 were synthesized from 2-nitroaniline or 2-amino-3- nitrophenol and tested for in vitro activity upon the intraerythrocytic stage of W2 and 3D7 Plasmodium falciparum strains. Biol. results showed good antimalarial activity with IC50 ranging from 0.3 to 21.1 μM. In attempting to investigate the large broad-spectrum antiprotozoal activities of these pyrrolo[1,2-a]quinoxaline derivatives, their properties toward the promastigote form of Leishmania donovani were also investigated and revealed their selective antiplasmodial profile. In parallel, the in vitro cytotoxicity of these mols. was assessed on the human HepG2 cell line. Structure-activity relationships of these new synthetic compounds are here discussed. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).HPLC of Formula: 5455-98-1

The Article related to antimalarial msbar, Pharmacology: Structure-Activity and other aspects.HPLC of Formula: 5455-98-1

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Toda, Yasunori; Tanaka, Katsumi; Matsuda, Riki; Suga, Hiroyuki published an article in 2019, the title of the article was Visible-light-triggered Catalytic Halohydrin Synthesis from Epoxides and Trichloroacetonitrile by Copper and Iron Salts.Related Products of 5455-98-1 And the article contains the following content:

Preparation of vicinal halohydrins by the ring-opening reaction of epoxides under visible-light conditions using copper or iron chlorides catalyst was described. The use of trichloroacetonitrile as a chloride source enabled catalytic HCl generation under the mild conditions. This method can also be applied to the aziridine ring-opening reaction. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Related Products of 5455-98-1

The Article related to epoxide trichloroacetonitrile metal chloride catalyst regioselective photochem ring opening, chlorohydrin preparation, Aliphatic Compounds: Alcohols and Thiols and other aspects.Related Products of 5455-98-1

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On February 18, 2022, Ondari, Mark E.; Klosin, Jerzy; Kruper, William R.; Lysenko, Ivan; Thomas, Pulikkottil J.; Cheng, Kevin; Abboud, Khalil A.; Kruper, William J. published an article.Quality Control of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the article was Diol-Ritter Reaction: Regio- and Stereoselective Synthesis of Protected Vicinal Aminoalcohols and Mechanistic Aspects of Diol Monoester Disproportionation. And the article contained the following:

Herein, a mechanism-based study of the less known diol-Ritter reaction had provided a highly regioselective procedure for the synthesis of 1-vic-amido-2-esters from either terminal epoxides or 1,2-diols via Lewis Acid-catalyzed monoesterification. When treated with stoichiometric Lewis Acid catalyst (BF3), these diol monoesters form dioxonium cation intermediates that are ring-opened with nitrile nucleophiles to form nitrilium intermediates, which undergo rapid and irreversible hydration to give the desired amidoesters. Diester byproduct formation was irreversible and appears to occur through a disproportionation of diol monoester. With chiral epoxide starting materials, the formation of amidoester occurs with retention of configuration and no apparent erosion of optical purity as determined by single-crystal X-ray analyzes and chiral chromatog., resp. The direct access to chiral vic-amidoesters was especially practical with regard to the synthesis of Gram-pos., antibacterial, oxazolidinone analogs of the Zyvox antimicrobial family. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Quality Control of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to protected vicinal aminoalc regioselective stereoselective preparation, General Organic Chemistry: Synthetic Methods and other aspects.Quality Control of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

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On August 16, 2019, Xu, Jian-Xing; Wu, Xiao-Feng published an article.Synthetic Route of 5455-98-1 The title of the article was Cobalt-Catalyzed Alkoxycarbonylation of Epoxides to 尾-Hydroxyesters. And the article contained the following:

Herein, the authors developed a new and practical catalytic system for the carbonylative synthesis of 尾-hydroxyesters. By using simple, cheap, and air-stable cobalt(II) bromide as the catalyst, combined with pyrazole and catalytic amount of manganese, active cobalt complex can be generated in situ and can catalyze various epoxides to give the corresponding 尾-hydroxyesters in moderate to excellent yields. Mechanism studies indicate that pyrazole plays a crucial role in this reaction. Moreover, with the addition of the catalytic amount of manganese, the active cobalt catalyst can be regenerated, which provides a possibility for reusing the cobalt catalyst. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Synthetic Route of 5455-98-1

The Article related to hydroxyester beta preparation cobalt catalyst epoxide alkoxycarbonylation, General Organic Chemistry: Synthetic Methods and other aspects.Synthetic Route of 5455-98-1

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Li, Dan-Dan; Niu, Liang-Feng; Ju, Zhi-Yu; Xu, Zhihong; Wu, Changzeng published an article in 2016, the title of the article was Palladium-Catalyzed C(sp2)-H Bond Alkylation of Ketoximes by Using the Ring-Opening of Epoxides.Electric Literature of 5455-98-1 And the article contains the following content:

A palladium-catalyzed ortho-directed alkylation of O-Me ketoximes that proceeds through a regioselective ring-opening reaction of epoxides has been demonstrated. This C(sp2)-H activation/alkylation protocol was carried out in pivalic acid/1,1,1,3,3,3-hexafluoro-2-propanol (PivOH/HFIP, 2:8) as the solvent and was applied to various O-Me ketoximes that contain either electron-donating or electron-withdrawing groups. Moreover, different types of epoxides were used in this alkylation reaction, which proceeded smoothly to give the corresponding products in moderate to good yields. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Electric Literature of 5455-98-1

The Article related to regioselective palladium catalyst alkylation ketoxime ring opening epoxide, General Organic Chemistry: Synthetic Methods and other aspects.Electric Literature of 5455-98-1

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On December 17, 2020, Borchardt, Allen; Brady, Thomas P.; Chen, Zhi-Yong; Do, Quyen-Quyen Thuy; Jiang, Wanlong; Tari, Leslie W. published a patent.Computed Properties of 5455-98-1 The title of the patent was Compositions and methods for the treatment of human immunodeficiency virus. And the patent contained the following:

Compositions and methods for the treatment of viral infections include conjugates containing inhibitors of viral gp120 receptor (e.g., temsavir, BMS-818251, DMJ-ll-121, BNM-IV-147, or analogs thereof) linked to an Fc monomer, an Fc domain, and Fc-binding peptide, an albumin protein, or albumin- binding peptide. In particular, conjugates can be used in the treatment of viral infections (e.g., HIV infections). The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Computed Properties of 5455-98-1

The Article related to composition treatment human hiv antiviral immunosuppression conjugate drug antibody, Pharmaceuticals: Formulation and Compounding and other aspects.Computed Properties of 5455-98-1

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On May 20, 2015, Pant, Kritee; Groeger, Dominic; Bergmann, Ralf; Pietzsch, Jens; Steinbach, Joerg; Graham, Bim; Spiccia, Leone; Berthon, Fannely; Czarny, Bertrand; Devel, Laurent; Dive, Vincent; Stephan, Holger; Haag, Rainer published an article.Reference of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the article was Synthesis and Biodistribution Studies of 3H- and 64Cu-Labeled Dendritic Polyglycerol and Dendritic Polyglycerol Sulfate. And the article contained the following:

Dendritic polyglycerol sulfate (dPGS) is a biocompatible, bioactive polymer which exhibits anti-inflammatory activity in vivo and thus represents a promising candidate for therapeutic and diagnostic applications. To investigate the in vivo pharmacokinetics in detail, dPGS with a mol. weight of approx. 10 kDa was radiolabeled with 3H and 64Cu, and evaluated by performing biodistribution studies and small animal positron emission tomog. (PET). 3H-labeling was accomplished by an oxidation-reduction process with sodium periodate and [3H]-borohydride. 64Cu-labeling was achieved by conjugation of isothiocyanate- or maleimide-functionalized copper(II)-chelating ligands based on 1,4-bis(2-pyridinylmethyl)-1,4,7-triazacyclononane (DMPTACN) to an amino functionalized dPGS scaffold, followed by reaction with an aqueous solution containing 64CuCl2. Independent biodistribution by radioimaging and PET imaging studies with healthy mice and rats showed that the neutral dPG was quant. renally eliminated, whereas the polysulfated analogs accumulated mainly in the liver and spleen. Small amounts of the dPGS derivatives were slowly excreted via the kidneys. The degree of uptake by the reticuloendothelial system (RES) was similar for dPGS with 40% or 85% sulfation, and surface modification of the scaffold with the DMPTACN chelator did not appear to significantly affect the biodistribution profile. On the basis of our data, the applicability of bioactive dPGS as a therapeutic agent might be limited due to organ accumulation even after 3 wk. The inert characteristics and clearance of the neutral polymer, however, emphasizes the potential of dPG as a multifunctional scaffold for various nanomedical applications. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Reference of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to tritium copper 64 dendrimer polyglycerol sulfate chelator biodistribution preparation, Pharmaceuticals: Formulation and Compounding and other aspects.Reference of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

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