Day: February 23, 2023

Design, synthesis and application of a new type of bifunctional Le-Phos in highly enantioselective γ-addition reactions of N-centered nucleophiles to allenoates was written by Qiu, Haile;Chen, Xiaofeng;Zhang, Junliang. And the article was included in Chemical Science in 2019.Recommanded Product: 5,5-Dimethyloxazolidin-2-one This article mentions the following:

A novel class of cyclic phosphine derived bifunctional catalysts (R_P,S,S,R_S)/(S_P,R,S,R_S)-Le-Phos I (R = Ph, pentafluorophenyl, cyclopentyl, etc.) is reported, which can be readily prepared from inexpensive and com. available starting materials and exhibit good performances in enantioselective γ-addition reactions of N-centered nucleophiles e.g., 1,3-oxazolidin-2-one and allenoates R¹CH=C=CHC(O)OR² (R¹ = Me, Et, cyclopentyl, etc.; R² = Et, tert-Bu, 4-fluorophenyl, etc.) under mild conditions. The salient features of this reaction include high product yields, good enantioselectivity, mild reaction conditions, and broad substrate scope and gram-scale scalability. In the experiment, the researchers used many compounds, for example, 5,5-Dimethyloxazolidin-2-one (cas: 1121-83-1Recommanded Product: 5,5-Dimethyloxazolidin-2-one).

5,5-Dimethyloxazolidin-2-one (cas: 1121-83-1) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries.Recommanded Product: 5,5-Dimethyloxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Formulation and evaluation of mouth dissolving film of Zolmitriptan by using natural polymers was written by Daswadkar, Shubhangi;Patil, Shivani B. Sontakke. And the article was included in World Journal of Pharmacy and Pharmaceutical Sciences in 2020.Application of 139264-17-8 This article mentions the following:

Zolmitriptan is a BCS class III generation antimigraine drug that is used for the treatment of migraine and has low metabolism and permeability. This drug also undergoes first-pass metabolism To overcome all these problems mouth dissolving films were prepared which helps to improve the bioavailability of drugs. Mouth films dissolve fastly along with drugs and mostly all the drug absorbs through oral mucosa in the systemic circulation. Mouth films were prepared by the solvent casting method. Various issues related to drug release and side effects of synthetic polymers, formulating mouth dissolving films of Zolmitriptan utilizing natural polymers was beneficial and effective, and its the main aim of present work. Polymer concentration, Glycerol, and type of polymer i.e. maize starch, pectin and guar gum were optimized by using central composite 3 factors, 2 level design based on drug release, and folding endurance of films. A total of 39 batches were prepared from which batch containing 50% pectin and 20% glycerol, was found to be best with desirability 0.998. Oral films of the optimized batch show 27±2 number of folds and show 98.12±0.1% drug release. The optimized film was further evaluated for drug content uniformity, phys. appearance, solubility, stability, disintegration and dissolution study. In the experiment, the researchers used many compounds, for example, (S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one (cas: 139264-17-8Application of 139264-17-8).

(S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one (cas: 139264-17-8) belongs to oxazolidine derivatives. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries. Chiral oxazolidines are widely used as chiral auxiliaries, chiral ligands, protecting and/or directing groups in a variety of asymmetric transformations, thanks also to their easy cleavage or their further elaboration possibilities.Application of 139264-17-8

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Regioselective C-H Thioarylation of Electron-Rich Arenes by Iron(III) Triflimide Catalysis was written by Dodds, Amy C.;Sutherland, Andrew. And the article was included in Journal of Organic Chemistry in 2021.HPLC of Formula: 1665-48-1 This article mentions the following:

A mild and regioselective method for the preparation of unsym. biaryl sulfides using iron(III) catalysis is described. Activation of N-(arylthio)succinimides using the powerful Lewis acid iron(III) triflimide allowed the efficient thiolation of a range of arenes, including anisoles, phenols, acetanilides, and N-heterocycles. The method was applicable for the late-stage thiolation of tyrosine and tryptophan derivatives and was used as the key step for the synthesis of pharmaceutically relevant biaryl sulfur-containing compounds such as the antibiotic dapsone and the antidepressant vortioxetine. Kinetic studies revealed that while N-(arylthio)succinimides bearing electron-deficient arenes underwent thioarylation catalyzed entirely by iron(III) triflimide, N-(arylthio)succinimides with electron-rich arenes displayed an autocatalytic mechanism promoted by the Lewis basic product. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1HPLC of Formula: 1665-48-1).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Oxazolidines are commonly used as metal ligands in asymmetric catalysis, synthetic intermediates in organic synthesis, and also used as the protecting groups.HPLC of Formula: 1665-48-1

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Diastereoselective synthesis of deprotectable isoxazolidines was written by Wang, Wentian;Rein, Kathleen S.. And the article was included in Tetrahedron Letters in 2013.COA of Formula: C6H7NO3 This article mentions the following:

Isoxazolidines are important synthetic targets due to their ability to act as nucleoside analogs. The 1,3-dipolar cycloaddition reaction of nitrones with alkenes is a powerful approach to the synthesis of isoxazolidines with the potential for control over absolute and relative stereoselectivity. However, removal of the most commonly used protecting groups without cleavage of the N-O bond is a significant challenge. The diastereoselective synthesis of benzhydryl protected isoxazolidines and the reductive cleavage of the benzhydryl protecting group with retention of the isoxazolidine ring are reported. In the experiment, the researchers used many compounds, for example, 3-Acryloyloxazolidin-2-one (cas: 2043-21-2COA of Formula: C6H7NO3).

3-Acryloyloxazolidin-2-one (cas: 2043-21-2) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Oxazolidines are cyclic condensation products of β-amino alcohols and aldehydes or ketone, and they undergo a facile and complete hydrolysis in aqueous solution. Alterations in carbonyl moiety control the rate of formation of a given β-amino alcohol.COA of Formula: C6H7NO3

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Sustained release of peptides and proteins from polymeric nanocarriers produced by inverse Flash NanoPrecipitation was written by Markwalter, Chester E.;Pagels, Robert F.;Hejazi, Ava N.;Ristroph, Kurt D.;Wang, Jiping;Chen, Ke;Li, Jian;Prud′homme, Robert K.. And the article was included in Journal of Controlled Release in 2021.Recommanded Product: 13590-42-6 This article mentions the following:

Peptide and protein therapeutics generally exhibit high potency and specificity and are increasingly important segments of the pharmaceutical market. However, their clin. applications are limited by rapid clearance and poor membrane permeability. Encapsulation of the peptide or protein into a nano-scale carrier can modify its pharmacokinetics and biodistribution. This might be employed to promote uptake in desired cell types or tissues, to limit systemic exposure, or to reduce the need for frequent injections. We have recently described inverse Flash NanoPptn. (iFNP), a scalable technique to encapsulate water-soluble therapeutics into polymeric nanocarriers, and have demonstrated improvements in therapeutic loading of an order of magnitude over comparable approaches. Here, we describe the formulation parameters that control release rates of encapsulated model therapeutics polymyxin B, lysozyme, and bovine serum albumin from nanocarriers produced using iFNP. Using a neutropenic lung infection mouse model with a multi-drug resistant Acinetobacter baumannii clin. isolate, we demonstrate enhanced therapeutic effect and safety profile afforded by nanocarrier-encapsulated polymyxin B following pulmonary administration. The encapsulated formulation reduced toxicity observed at elevated doses and resulted in up to 2.7-log10 reduction in bacterial burden below that of unencapsulated polymyxin B. These results establish the promise of iFNP as a platform for nanocarrier delivery of water-soluble therapeutics. In the experiment, the researchers used many compounds, for example, (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate (cas: 13590-42-6Recommanded Product: 13590-42-6).

(S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate (cas: 13590-42-6) belongs to oxazolidine derivatives. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries. Oxazolidines are cyclic condensation products of β-amino alcohols and aldehydes or ketone, and they undergo a facile and complete hydrolysis in aqueous solution. Alterations in carbonyl moiety control the rate of formation of a given β-amino alcohol.Recommanded Product: 13590-42-6

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Impact of COVID-19 pandemic on migraine management in the United States: insights from migraine tracking app users was written by Kato, Yuji;Poh, Weijie;Horvath, Zsolt;Cadiou, Francois;Shimazu, Tomokazu;Maruki, Yuichi. And the article was included in BMC Neurology in 2021.Related Products of 139264-17-8 This article mentions the following:

The nature of COVID-19 pandemic measures has altered the clin. management of migraine, and has also created barriers to evaluate the impact of such measures of migraine patients. Using the Migraine Buddy smartphone application, we assessed the impact of the COVID-19 pandemic on migraine in users residing in the United States. Migraine Buddy is a smartphone application by individuals to record their migraine headache episodes, characteristics, and coping mechanisms. For this study, anonymized self-reported data from 163,176 adult Migraine Buddy users in the United States between Jan. 2020 and May 2020, were analyzed for migraines associated with stress. A stress-related migraine is defined as one in which stress or anxiety was reported as a trigger or symptom. A questionnaire on the impact of COVID-19 on migraine and its management was also completed by 923 users from the United States in the app between Apr. 2020 and May 2020. 88% Of the Migraine Buddy database extract and 84% of the respondents are female, with a mean age of 36.2 years. The proportion of stress-related migraine attacks peaked at 53% on March 21 to 23, although the number of migraine attacks decreased. This followed the declaration of the COVID-19 national emergency on March 13 and a spike in the number of COVID-19 cases in the United States. Questionnaire respondents felt that the following added more stress: social isolation (22.6%), information overdose (21.2%), access to essentials (food, medication, etc.) (18.7%), and financial concerns (17.8%). To help manage migraine during COVID-19, respondents suggested stress and diet coaching programs and resources (medical articles, etc.) (34.0%), having the option for home delivery of medication (30.6%) and tele-consulting (25.5%). Here, we report the change in the proportion of self-reported stress-related migraine in relation to evolution of the COVID-19 pandemic, as well as its impact of migraine management. Our data will help increase the understanding of patients’ needs and help with planning and execution of mitigating strategies. In the experiment, the researchers used many compounds, for example, (S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one (cas: 139264-17-8Related Products of 139264-17-8).

(S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one (cas: 139264-17-8) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Some reports highlighted again the effectiveness of oxazolidine-based compounds in driving the stereo- or diastereotopic outcome of chemical reactions.Related Products of 139264-17-8

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Copper-Mediated Selective Cross-Coupling of 1,1-Dibromo-1-alkenes and Heteronucleophiles: Development of General Routes to Heterosubstituted Alkynes and Alkenes was written by Jouvin, Kevin;Coste, Alexis;Bayle, Alexandre;Legrand, Frederic;Karthikeyan, Ganesan;Tadiparthi, Krishnaji;Evano, Gwilherm. And the article was included in Organometallics in 2012.Name: 3-(Phenylethynyl)oxazolidin-2-one This article mentions the following:

Efficient and general procedures for the cross-coupling of 1,1-dibromoalkenes and N-, O-, and P-nucleophiles are reported. Fine-tuning of the reaction conditions allows for either site-selective, double, or alkynylative cross-coupling, therefore providing divergent and straightforward entries to numerous building blocks such as bromoenamides, ynamides, ketene N,N-acetals, bromoenol ethers, ynol ethers, ketene O,O-acetals, or vinylphosphonates and further expanding the copper catalysis toolbox with useful and versatile processes. In the experiment, the researchers used many compounds, for example, 3-(Phenylethynyl)oxazolidin-2-one (cas: 888329-88-2Name: 3-(Phenylethynyl)oxazolidin-2-one).

3-(Phenylethynyl)oxazolidin-2-one (cas: 888329-88-2) belongs to oxazolidine derivatives. A common way to produce multisubstituted oxazolidines is by means of cycloaddition reactions. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries.Name: 3-(Phenylethynyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Direct β-Alkylation of Aldehydes via Photoredox Organocatalysis was written by Terrett, Jack A.;Clift, Michael D.;MacMillan, David W. C.. And the article was included in Journal of the American Chemical Society in 2014.Product Details of 2043-21-2 This article mentions the following:

In the presence of a bis(C,N-dimethylphenylpyridinyl)(di-tert-butylbipyridinyl)iridium(III) complex as a photocatalyst and dicyclohexylamine as an organocatalyst, aldehydes such as octanal underwent chemoselective photochem. β-alkylation with electron-deficient alkenes such as H₂C:CRR¹ (R = H, Ph, 1-naphthyl, 4-MeOC₆H₄, 4-FC₆H₄, 4-ClC₆H₄, 2-BrC₆H₄; R¹ = PhCH₂O₂C, MeO₂C, NC, PhSO₂, 2-oxo-3-oxazolidinylcarbonyl) under blue LED light to give β-substituted aldehydes such as OHCCH₂CH(CH₂Bu)CH₂CHRR¹ (R = H, Ph, 1-naphthyl, 4-MeOC₆H₄, 4-FC₆H₄, 4-ClC₆H₄, 2-BrC₆H₄; R¹ = PhCH₂O₂C, MeO₂C, NC, PhSO₂, 2-oxo-3-oxazolidinylcarbonyl) in 50-83% yields. The reaction used the photochem. oxidation of enamines generated from aldehydes to yield enaminyl radicals as the key step. A benzyl oxodecenoate and a benzyl oxononenoate underwent chemoselective and stereoselective cyclization under the alkylation conditions to yield oxoethylcycloalkylacetates in 54% and 47% yields. Fluorescence quenching and EPR studies were used to study the reaction mechanism. In the experiment, the researchers used many compounds, for example, 3-Acryloyloxazolidin-2-one (cas: 2043-21-2Product Details of 2043-21-2).

3-Acryloyloxazolidin-2-one (cas: 2043-21-2) belongs to oxazolidine derivatives. A common way to produce multisubstituted oxazolidines is by means of cycloaddition reactions. Some reports highlighted again the effectiveness of oxazolidine-based compounds in driving the stereo- or diastereotopic outcome of chemical reactions.Product Details of 2043-21-2

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Hydrogen bonding to metal β-ketoenolates was written by Davis, T. S.;Fackler, J. P. Jr.. And the article was included in Inorganic Chemistry in 1966.Quality Control of Bis(2,2′,6,6′-tetramethylheptanedionato) palladium(II) This article mentions the following:

An ir spectral examination of H bonding to various neutral bis, tris, and tetrakis β-ketoenolate complexes were carried out by using deuteriochloroform, H₂O, and MeOH as the H-bonding agents. Very weak or no H bonding with the tetrahedral bis complexes, stronger H bonding to the planar bis and to many of the tris complexes, and a pronounced interaction of the solvent with tetrakis complexes are indicated. The H-bond interaction of H₂O with acetylacetonatomanganese-(III) and diisobutyrylmethanatomanganese(III) also was examined Sites available for H bonding to the complexes are discussed. In the experiment, the researchers used many compounds, for example, Bis(2,2′,6,6′-tetramethylheptanedionato) palladium(II) (cas: 15214-66-1Quality Control of Bis(2,2′,6,6′-tetramethylheptanedionato) palladium(II)).

Bis(2,2′,6,6′-tetramethylheptanedionato) palladium(II) (cas: 15214-66-1) belongs to oxazolidine derivatives.Oxazolidines are readily available also from propargyl amines. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries.Quality Control of Bis(2,2′,6,6′-tetramethylheptanedionato) palladium(II)

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Dual pH/ROS-Responsive Nanoplatform with Deep Tumor Penetration and Self-Amplified Drug Release for Enhancing Tumor Chemotherapeutic Efficacy was written by Li, Yongfei;Chen, Mie;Yao, Bowen;Lu, Xun;Song, Boyang;Vasilatos, Shauna N.;Zhang, Xiang;Ren, Xiaomei;Yao, Chang;Bian, Weihe;Sun, Lizhu. And the article was included in Small in 2020.Application In Synthesis of (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate This article mentions the following:

Poor deep tumor penetration and incomplete intracellular drug release remain challenges for antitumor nanomedicine application in clin. settings. Herein, a nanomedicine (RLPA-NPs) is developed that can achieve prolonged blood circulation, deep tumor penetration, active-targeting of cancer cells, endosome/lysosome escape, and intracellular selectivity self-amplified drug release for effective drug delivery. The RLPA-NPs are constructed by encapsulation of a pH-sensitive polymer octadecylamine-poly(aspartate-1-(3-aminopropyl) imidazole) (OA-P(Asp-API)) and a ROS-generation agent, β-Lapachone (Lap), in micelles assembled by the tumor-penetration peptide internalizing RGD (iRGD)-modified ROS-responsive paclitaxel (PTX)-prodrug. iRGD could promote RLPA-NPs penetration into deep tumor tissue, and specific targeting to cancer cells. After internalization by cancer cells through receptor-mediated endocytosis, OA-P(Asp-API) can rapidly protonate in the endosome’s acidic environment, resulting in RLPA-NPs escape from the endosome through the “proton sponge effect”. At the same time, the RLPA-NPs micelle disassembles, releasing Lap and PTX-prodrug. Subsequently, the released Lap could generate ROS, consequently amplifying and accelerating PTX release to kill tumor cells. The in vitro and in vivo studies demonstrated that RLPA-NPs can significantly improve the therapeutic effect compared to control groups. Therefore, RLPA-NPs are a promising nanoplatform for overcoming multiple physiol. and pathol. barriers to enhance drug delivery. In the experiment, the researchers used many compounds, for example, (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate (cas: 13590-42-6Application In Synthesis of (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate).

(S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate (cas: 13590-42-6) belongs to oxazolidine derivatives. Oxazolidine-based compounds are well-known chiral auxiliaries and strategic molecular moieties in chemistry since they can effectively mask or mimic amino acid units or amino alcohols. As well as other multifunctional heterocyclic compounds, oxazolidine rings play an essential role in organic and medicinal chemistry, behaving, in some cases as powerful antitumor agents.Application In Synthesis of (S)-Benzyl 2-(2,5-dioxooxazolidin-4-yl)acetate

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem