Month: October 2022

Category: ethers-buliding-blocksIn 2020 ,《Recent advances regarding the therapeutic potential of adapalene》 appeared in Pharmaceuticals. The author of the article were Rusu, Aura; Tanase, Corneliu; Pascu, Georgiana-Andreea; Todoran, Nicoleta. The article conveys some information:

A review. Adapalene (ADP) is a representative of the third retinoids generation and successfully used in first-line acne treatment. ADP binds to retinoic acid nuclear receptors. The comedolytic, anti-inflammatory, antiproliferative, and immunomodulatory are the known ADP effects. Its safety profile is an advantage over other retinoids. ADP recently was found to be effective in the treatment of several dermatol. diseases and photoaging besides the utility in the treatment of acne vulgaris. New biol. effects of adapalene with therapeutic potential are highlighted in this review paper. Thus, adapalene could be a valuable therapeutic drug into the treatment of several types of cancer. Addnl., some neurodegenerative diseases could be treated with a suitable formulation for i.v. administration. The antibacterial activity against methicillin-resistant Staphylococcus aureus of an analog of ADP has been proven. In different therapeutic schemes, ADP is more effective in combination with other active substances. New topical combinations with adapalene include ketoconazole (antifungal), mometasone furoate (anti-inflammatory corticosteroid), nadifloxacin (fluoroquinolone), and alfa and beta hydroxy acids. Combination with oral drugs is a new trend that enhances the properties of topical formulations with adapalene. Several studies have investigated the effects of ADP in co-administration with azithromycin, doxycycline, faropenem, isotretinoin, and valganciclovir. Innovative formulations of ADP also aim to achieve a better bioavailability, increased efficacy, and reduced side effects. In this review, we have highlighted the current studies on adapalene regarding biol. effects useful in various treatment types. Adapalene has not been exploited yet to its full biol. potential. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: ethers-buliding-blocks)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Category: ethers-buliding-blocks

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HPLC of Formula: 673-22-3In 2022 ,《Recyclable palladium-catalyzed cyclocarbonylation between benzyl chlorides and salicylic aldehydes towards coumarins》 was published in Molecular Catalysis. The article was written by Zhou, Yan; Zhou, Zebiao; Liu, Siqi; Cai, Mingzhong. The article contains the following contents:

A novel and practical route to coumarin derivatives was developed via the heterogeneous Pd-catalyzed carbonylative reaction and subsequent intramol. condensation process starting from com. easily available benzyl chlorides and salicylic aldehydes. Reactions were performed in the existence of 2 mol% of an SBA-15-immobilized bidentate phosphine palladium complex [SBA-15-P,P-PdCl2] in dioxane at 110°C with Et3N as base under 10 bar of CO to afford a wide range of coumarin derivatives mostly with good to high yields. Importantly, this new heterogenized palladium complex was easy to recover via filtration of the reaction mixture, and was recyclable up to 8 times without apparent drop in its catalytic performance. After reading the article, we found that the author used 2-Hydroxy-4-methoxybenzaldehyde(cas: 673-22-3HPLC of Formula: 673-22-3)

2-Hydroxy-4-methoxybenzaldehyde(cas: 673-22-3) is the main component of root bark essential oil of Periploca sepium Bunge. It is a potential tyrosinase inhibitor present in African medicinal plants. 2-Hydroxy-4-methoxybenzaldehyde was used in the synthesis of Schiff base ligand.HPLC of Formula: 673-22-3

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Recommanded Product: 2-(Benzyloxy)acetaldehydeIn 2021 ,《Photoredox-catalyzed aminofluorosulfonylation of unactivated olefins》 was published in Chemical Science. The article was written by Zhong, Tao; Yi, Ji-Tao; Chen, Zhi-Da; Zhuang, Quan-Can; Li, Yong-Zhao; Lu, Gui; Weng, Jiang. The article contains the following contents:

The first three-component aminofluorosulfonylation of unactivated olefins, e.g., cyclohex-2-en-1-yl N-(4-chlorophenyl)carbamate by merging photoredox-catalyzed proton-coupled electron transfer (PCET) activation with radical relay processes has been described. Various aliphatic sulfonyl fluorides featuring a privileged 5-membered heterocyclic core compounds, e.g., I have been efficiently afforded under mild conditions with good functional group tolerance. The synthetic potential of the sulfonyl fluoride products has been examined by diverse transformations including SuFEx reactions and transition metal-catalyzed cross-coupling reactions. Mechanistic studies demonstrate that amidyl radicals, alkyl radicals and sulfonyl radicals are involved in this difunctionalization transformation. In the experiment, the researchers used 2-(Benzyloxy)acetaldehyde(cas: 60656-87-3Recommanded Product: 2-(Benzyloxy)acetaldehyde)

2-(Benzyloxy)acetaldehyde(cas: 60656-87-3) is a non-natural aldehyde. It undergoes enantioselective Mukaiyama aldol reaction with silylketene acetal nucleophiles in the presence of C2-symmetric bis(oxazolinyl)pyridine Cu(II) complex (catalyst).Recommanded Product: 2-(Benzyloxy)acetaldehyde

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Ether – Wikipedia,
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HPLC of Formula: 150-19-6In 2020 ,《Enantioselective Synthesis of Tertiary α,α-Diaryl Carbonyl Compounds Using Chiral N,N’-Dioxides under Umpolung Conditions》 was published in Organic Letters. The article was written by Um, Tae-Woong; Lee, Girim; Shin, Seunghoon. The article contains the following contents:

Bronsted acid-catalyzed addition of the chiral N,N’-dioxide into ynamides generated enolonium ions in situ which underwent enantioselective alkylation by indoles, pyrroles, and phenols, without racemization of the formed tertiary center. This external oxidant approach allows for the use of unmodified nucleophiles and does not leave trace groups from the oxidant, which significantly increases the synthetic efficiency and the product diversity. Furthermore, the byproduct of the N,N’-dioxide could be efficiently recycled into an optically pure form. The results came from multiple reactions, including the reaction of m-Methoxyphenol(cas: 150-19-6HPLC of Formula: 150-19-6)

m-Methoxyphenol(cas: 150-19-6) may be used as an analytical standard for the determination of the analyte in wine, coffee beans, wood samples, and mainstream smoke by gas chromatography (GC) based techniques.HPLC of Formula: 150-19-6

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Ether – Wikipedia,
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Name: 2-(Benzyloxy)acetaldehydeIn 2021 ,《Asymmetric Synthesis of Homoallylic Alcohols Featuring Vicinal Tetrasubstituted Carbon Centers via Dual Pd/Photoredox Catalysis》 was published in Organic Letters. The article was written by Xue, Sijing; Limburg, Bart; Ghorai, Debasish; Benet-Buchholz, Jordi; Kleij, Arjan W.. The article contains the following contents:

Dual palladium/photoredox-catalysis provides an effective method for the decarboxylative asym. synthesis of vicinal α,β-tri/tetra- or α,β-tetrasubstituted homoallylic alcs. using Hantzsch-type esters as radical precursors. This mild methodol. capitalizes on vinyl cyclic carbonates as accessible reagents providing the target mols. in appreciable to good yields, high branch selectivity, and enantiomeric ratios of up to 94:6, making it a rare example of using prochiral electrophiles for the creation of vicinal congested carbon centers. After reading the article, we found that the author used 2-(Benzyloxy)acetaldehyde(cas: 60656-87-3Name: 2-(Benzyloxy)acetaldehyde)

2-(Benzyloxy)acetaldehyde(cas: 60656-87-3) is a non-natural aldehyde. It undergoes enantioselective Mukaiyama aldol reaction with silylketene acetal nucleophiles in the presence of C2-symmetric bis(oxazolinyl)pyridine Cu(II) complex (catalyst).Name: 2-(Benzyloxy)acetaldehyde

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Tri- and tetravalent photoactivable cross-linking agents》 was written by Welle, Alexandre; Billard, Francois; Marchand-Brynaert, Jacqueline. Related Products of 139115-91-6This research focused ontrivalent tetravalent photoactivable cross linking agent preparation. The article conveys some information:

A modular synthesis of photoactivable crosslinking agents is described, using an aromatic core, di- or triethyleneglycol spacers and photoaffinity labeling synthons that feature either perfluorophenyl azide or aryl(trifluoromethyl)diazirine motifs. Sym. and nonsym. trivalent structures, e.g. I [L = CH2CH2OCH2CH2NH], were obtained from phloroglucinol and dopamine, resp. Sym. tetravalent structures resulted from the coupling of two dopamine derivatives with oxalyl chloride. The experimental process involved the reaction of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Related Products of 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly. Related Products of 139115-91-6

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2021,CCS Chemistry included an article by Tang, Xiaowen; Luo, Xiang; Su, Qiong; Wei, Gaofei; Meng, Shan-Shui; Chan, Albert S. C.. Name: 2-Hydroxy-2-(4-propoxyphenyl)acetic acid. The article was titled 《Chemoselective dual functionalization of phenols via relay catalysis of borane with different forms》. The information in the text is summarized as follows:

A highly efficient and chemoselective dual functionalization of unprotected phenols with α- or β- hydroxyl acids was presented. A variety of valuable benzofuranones and dihydrocoumarins were delivered in moderate to high yields. D. functional theory (DFT) calculations and control experiments indicated that an untypical Friedel-Crafts alkylation and the subsequent lactonization were catalyzed by the Lewis acid form and the Bronsted acid form of borane, resp. Gram-scale experiments and late-stage functionalization of complex mols. were performed to highlight the utility of this reaction. In the experiment, the researchers used many compounds, for example, 2-Hydroxy-2-(4-propoxyphenyl)acetic acid(cas: 79694-16-9Name: 2-Hydroxy-2-(4-propoxyphenyl)acetic acid)

2-Hydroxy-2-(4-propoxyphenyl)acetic acid(cas: 79694-16-9) belongs to ethers.Oxygen is more electronegative than carbon, thus the alpha hydrogens of ethers are more acidic than those of simple hydrocarbons. They are far less acidic than alpha hydrogens of carbonyl groups (such as in ketones or aldehydes), however. Name: 2-Hydroxy-2-(4-propoxyphenyl)acetic acid

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2014,Zhang, Hong-Wu; Wang, Li-Qin; Xiang, Qing-Feng; Zhong, Qian; Chen, Lu-Ming; Xu, Cai-Xia; Xiang, Xian-Hong; Xu, Bo; Meng, Fei; Wan, Yi-Qian; Deng, David Y. B. published 《Specific lipase-responsive polymer-coated gadolinium nanoparticles for MR imaging of early acute pancreatitis》.Biomaterials published the findings.Product Details of 139115-91-6 The information in the text is summarized as follows:

Currently, available methods for diagnosis of acute pancreatitis (AP) are mainly dependent on serum enzyme anal. and imaging techniques that are too low in sensitivity and specificity to accurately and promptly diagnose AP. The lack of early diagnostic tools highlights the need to search for a highly effective and specific diagnostic method. In this study, we synthesized a conditionally activated, gadolinium-containing, nanoparticle-based MRI nanoprobe as a diagnostic tool for the early identification of AP. Gadolinium diethylenetriaminepentaacetic fatty acid (Gd-DTPA-FA) nanoparticles were synthesized by conjugation of DTPA-FA ligand and gadolinium acetate. Gd-DTPA-FA exhibited low cytotoxicity and excellent biocompatibility when characterized in vitro and in vivo studies. L-arginine induced a gradual increase in the intensity of the T1-weighted MRI signal from 1 h to 36 h in AP rat models. The increase in signal intensity was most significant at 1 h, 6 h and 12 h. These results suggest that the Gd-DTPA-FA as an MRI contrast agent is highly efficient and specific to detect early AP. After reading the article, we found that the author used tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Product Details of 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. Product Details of 139115-91-6 They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2019,Oncologist included an article by Chayahara, Naoko; Mukohara, Toru; Tachihara, Motoko; Fujishima, Yoshimi; Fukunaga, Atsushi; Washio, Ken; Yamamoto, Masatsugu; Nakata, Kyosuke; Kobayashi, Kazuyuki; Takenaka, Kei; Toyoda, Masanori; Kiyota, Naomi; Tobimatsu, Kazutoshi; Doi, Hisayo; Mizuta, Naomi; Marugami, Naho; Kawaguchi, Atsushi; Nishigori, Chikako; Nishimura, Yoshihiro; Minami, Hironobu. COA of Formula: C28H28O3. The article was titled 《Adapalene gel 0.1% versus placebo as prophylaxis for anti-epidermal growth factor receptor-induced acne-like rash: A randomized left-right comparative evaluation (APPEARANCE)》. The information in the text is summarized as follows:

The results of the APPEARANCE trial indicate that adapalene does not prevent acne-like rash over placebo when added to topical moisturizer and oral minocycline but instead may have a detrimental effect. Therefore, adapalene is not recommended as prophylaxis against acne-like rash induced by anti-epidermal growth factor receptor therapies. Given that acne-like rash was completely controlled with placebo in approx. half of patients, predictive measures to identify patients needing intensive prophylaxis are required. Anti-epidermal growth factor receptor (EGFR) therapies are frequently associated with acne-like rash. To evaluate the prophylactic efficacy of adapalene, a topical retinoid used as first-line therapy for acne vulgaris, we conducted a randomized, placebo-controlled, evaluator-blinded, left-right comparative trial. Patients with non-small cell lung, colorectal, or head and neck cancer scheduled to receive anti-EGFR therapies were randomly assigned to once-daily adapalene application on one side of the face, with placebo on the other side. All patients had topical moisturizer coapplied to both sides of the face, and received oral minocycline. The primary endpoint was the difference in total facial lesion count of acne-like rash at 4 wk. Secondary endpoints included complete control rate (CCR) of acne-like rash (≤5 facial lesions) and global skin assessment (Investigator’s Global Assessment [IGA] scale, grade 0-4) at 4 wk. Two blinded dermatologists independently evaluated the endpoints from photographs. A total of 36 patients were enrolled, of whom 26 were evaluable. Adapalene treatment was associated with a greater lesion count than placebo at 4 wk, although the difference was not statistically significant (mean, 12.6 vs. 9.8, p = .12). All four patients with a difference >10 in lesion count between face sides had a greater count on the adapalene-treated side. No significant differences were observed in CCR of acne-like rash (54% vs. 50%) or IGA scale (mean grade, 1.9 vs. 1.7) between the adapalene and placebo sides. Adapalene is not recommended as prophylaxis against acne-like rash induced by anti-EGFR therapies. The experimental part of the paper was very detailed, including the reaction process of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9COA of Formula: C28H28O3)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.COA of Formula: C28H28O3

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2019,ChemistrySelect included an article by Jori, Popat K.; Jadhav, Vrushali H.. Safety of 1-Iodo-2-methoxybenzene. The article was titled 《Transition-Metal-Free Glucose-Derived Carbonaceous Catalyst Catalyzes Direct C-H Arylation of Unactivated Arenes with Aryl Halides》. The information in the text is summarized as follows:

The metal free catalyst by a very simple, economical and greener method was prepared The green catalyst showed remarkable activity in developing a simple and efficient method for C-H arylation of benzene with number of aryl halides RI (R = 3-methylphenyl, 4-chlorophenyl, naphth-1-yl, biphenyl-4-yl, etc.) in the synthesis of biaryls RC6H5. This method can be used to generate a diverse range of biaryl’s in good to excellent yields. The experimental process involved the reaction of 1-Iodo-2-methoxybenzene(cas: 529-28-2Safety of 1-Iodo-2-methoxybenzene)

1-Iodo-2-methoxybenzene(cas: 529-28-2) is a useful synthetic intermediate. It can be used in the synthesis of piperidinyl diaminopyrimidines as cyclin-dependent kinase inhibitors with antitumor activity and polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth.Safety of 1-Iodo-2-methoxybenzene

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Ether – Wikipedia,
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