Month: November 2022

Related Products of 2240-88-2On October 8, 2021 ,《Synthesis of N-(2-SF5-ethyl)amines and impact of the SF5 substituent on their basicity and lipophilicityã€?was published in Tetrahedron. The article was written by Gilbert, Audrey; Langowski, Pauline; Paquin, Jean-Francois. The article contains the following contents:

The synthesis of N-(2-SF5-ethyl)amines e.g., I is reported via the SN2 reaction between various amines, e.g., Me (2S)-pyrrolidine-2-carboxylate and 2-(pentafluoro-λ6-sulfanyl)ethyl trifluoromethanesulfonate as the SF5-containing electrophile. A total of 14 examples of SF5-containing aliphatic amines were synthesized, with yields going from 19 to 92%. Moreover, the effect of the SF5 substituent on the basicity and the lipophilicity of the amine was evaluated, and the SF5 group showed to decrease both the pKaH and the log D (pH = 7.0) values.3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2Related Products of 2240-88-2) was used in this study.

3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2) is a important organic intermediate. It can be used in agrochemical, pharmaceutical and dyestuff field.Related Products of 2240-88-2

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SDS of cas: 23828-92-4On May 1, 2020 ,《Combination of large volume sample stacking with polarity switching and cyclodextrin electrokinetic chromatography (LVSS-PS-CDEKC) for the determination of selected preservatives in pharmaceuticalsã€?appeared in Talanta. The author of the article were Pieckowski, Michal; Kowalski, Piotr; Baczek, Tomasz. The article conveys some information:

In this study, a large volume sample stacking (LVSS) with polarity switching (PS) and cyclodextrin electrokinetic chromatog. (CDEKC) method has been developed for the simultaneous separation and determination of 8 preservatives: methylparaben (MP), ethylparaben (EP), propylparaben (PP), butylparaben (BP), isobutylparaben (IBP), sorbic acid (SA), benzoic acid (BA), p-hydroxybenzoic acid (PHBA) in pharmaceuticals. The effects of some typical parameters such as sample volume, applied voltage, composition and pH of the running buffer and organic modifier concentration were examined and optimized. Moreover, the impact of type and concentration of cyclodextrin as electrolyte modifiers was also investigated. The detection limits of analytes for the elaborated LVSS-PS-CDEKC method were found to be in 0.8-5 ng mL-1 range, which were around 500 times lower than normal CDEKC without preconcentration technique. All analytes were completely resolved in less than 11 min in an uncoated fused-silica capillary of 75μm internal diameter (I.D) x 50 cm length. The electrophoretic separation was performed in a 2 mM α-cyclodextrin and 25 mM tetraborate system (pH = 9.3) with an applied voltage of 25 kV. The established method was validated and confirmed to be applicable for the determination of the preservatives in a quality control of pharmaceuticals.trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4SDS of cas: 23828-92-4) was used in this study.

trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4) enhances pulmonary surfactant production and stimulates ciliary activity.SDS of cas: 23828-92-4 It promotes mucus clearance, facilitates expectoration and eases productive cough, allowing patients to breathe.

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He, Yu-Tao; Li, Li-Xuan; Lin, Xiaohong; Hou, Bao-Long; Li, Chuang-Chuang published an article on January 14 ,2022. The article was titled 《Synthesis of Various Bridged Ring Systems via Rhodium-Catalyzed Bridged (3+2) Cycloadditionsã€? and you may find the article in Organic Letters.Application of 57044-25-4 The information in the text is summarized as follows:

Here, the authors describe the rhodium-catalyzed bridged [3+2]-cycloaddition cascade reactions of N-sulfonyl-1,2,3-triazoles, which allowed the efficient diastereoselective construction of various functionalized and synthetically challenging bridged ring systems. This simple, direct transformation had a broad substrate scope and excellent functional group tolerance. The highly strained polycyclic bicyclo[2.2.2]octa[b]indole core of fruticosine was synthesized efficiently using this methodol. The experimental process involved the reaction of (R)-Oxiran-2-ylmethanol(cas: 57044-25-4Application of 57044-25-4)

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Application of 57044-25-4

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In 2020,Molecules included an article by Moriyama, Mizuki; Nakata, Kohei; Fujiwara, Tetsuya; Tanabe, Yoo. Category: alcohols-buliding-blocks. The article was titled 《Divergent asymmetric total synthesis of all four pestalotin diastereomers from (R)-glycidolã€? The information in the text is summarized as follows:

All four chiral pestalotin diastereomers were synthesized in a straightforward and divergent manner from common (R)-glycidol. Catalytic asym. Mukaiyama aldol reactions of readily-available bis(TMSO)diene (Chan’s diene) with (S)-2-benzyloxyhexanal derived from (R)-glycidol produced a syn-aldol adduct with high diastereoselectivity and enantioselectivity using a Ti(iOPr)4/(S)-BINOL/LiCl catalyst. Diastereoselective Mukaiyama aldol reactions mediated by catalytic achiral Lewis acids directly produced not only a (1’S,6S)-pyrone precursor via the syn-aldol adduct using TiCl4, but also (1’S,6R)-pyrone precursor via the antialdol adduct using ZrCl4, in a stereocomplementary manner. A Hetero-Diels-Alder reaction of similarly available mono(TMSO)diene (Brassard’s diene) with (S)-2-benzyloxyhexanal produced the (1’S,6S)-pyrone precursor promoted by Eu(fod)3 and the (1’S,6R)-pyrone precursor Et2AlCl. Debenzylation of the (1’S,6S)-precursor and the (1’S,6R)-precursor furnished natural (-)-pestalotin (99% ee, 7 steps) and unnatural (+)-epipestalotin (99% ee, 7 steps), resp. Mitsunobu inversions of the obtained (-)-pestalotin and (+)-epipestalotin successfully produced the unnatural (+)-pestalotin (99% ee, 9 steps) and (-)-epipestalotin (99% ee, 9 steps), resp., in a divergent manner. All four of the obtained chiral pestalotin diastereomers possessed high chem. and optical purities (optical rotations, 1H-NMR, 13C-NMR, and HPLC measurements). After reading the article, we found that the author used (R)-Oxiran-2-ylmethanol(cas: 57044-25-4Category: alcohols-buliding-blocks)

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Category: alcohols-buliding-blocks

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In 2021,PLoS One included an article by Nagata, Kenichiro; Tsuji, Toshikazu; Suetsugu, Kimitaka; Muraoka, Kayoko; Watanabe, Hiroyuki; Kanaya, Akiko; Egashira, Nobuaki; Ieiri, Ichiro. Product Details of 23828-92-4. The article was titled 《Detection of overdose and underdose prescriptions-An unsupervised machine learning approachã€? The information in the text is summarized as follows:

Overdose prescription errors sometimes cause serious life-threatening adverse drug events, while underdose errors lead to diminished therapeutic effects. Therefore, it is important to detect and prevent these errors. In the present study, we used the one-class support vector machine (OCSVM), one of the most common unsupervised machine learning algorithms for anomaly detection, to identify overdose and underdose prescriptions. We extracted prescription data from electronic health records in Kyushu University Hospital between Jan. 1, 2014 and Dec. 31, 2019. We constructed an OCSVM model for each of the 21 candidate drugs using three features: age, weight, and dose. Clin. overdose and underdose prescriptions, which were identified and rectified by pharmacists before administration, were collected. Synthetic overdose and underdose prescriptions were created using the maximum and min. doses, defined by drug labels or the UpToDate database. We applied these prescription data to the OCSVM model and evaluated its detection performance. We also performed comparative anal. with other unsupervised outlier detection algorithms (local outlier factor, isolation forest, and robust covariance). Twenty-seven out of 31 clin. overdose and underdose prescriptions (87.1%) were detected as abnormal by the model. The constructed OCSVM models showed high performance for detecting synthetic overdose prescriptions (precision 0.986, recall 0.964, and F-measure 0.973) and synthetic underdose prescriptions (precision 0.980, recall 0.794, and F-measure 0.839). In comparative anal., OCSVM showed the best performance. Our models detected the majority of clin. overdose and underdose prescriptions and demonstrated high performance in synthetic data anal. OCSVM models, constructed using features such as age, weight, and dose, are useful for detecting overdose and underdose prescriptions. In the part of experimental materials, we found many familiar compounds, such as trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4Product Details of 23828-92-4)

trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4) is a medication indicated to alleviate chest congestion associated with conditions that include bronchitis, pneumonia, bronchospasm asthma, cough, and allergy.Product Details of 23828-92-4 Preclinically, ambroxol, the active ingredient of Mucosolvan, has been shown to increase respiratory tract secretion.

Referemce:
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Rakauskaite, Rasa; Urbanaviciute, Giedre; Simanavicius, Martynas; Lasickiene, Rita; Vaitiekaite, Ausra; Petraityte, Grazina; Masevicius, Viktoras; Zvirbliene, Aurelija; Klimasauskas, Saulius published their research in iScience on December 18 ,2020. The article was titled 《Photocage-Selective Capture and Light-Controlled Release of Target Proteinsã€?Synthetic Route of C8H9NO5S The article contains the following contents:

Photochem. transformations enable exquisite spatiotemporal control over biochem. processes; however, methods for reliable manipulations of biomols. tagged with biocompatible photo-sensitive reporters are lacking. Here we created a high-affinity binder specific to a photolytically removable caging group. We utilized chem. modification or genetically encoded incorporation of noncanonical amino acids to produce proteins with photocaged cysteine or selenocysteine residues, which were used for raising a high-affinity monoclonal antibody against a small photoremovable tag, 4,5-dimethoxy-2-nitrobenzyl (DMNB) group. Employing the produced photocage-selective binder, we demonstrate selective detection and immunoprecipitation of a variety of DMNB-caged target proteins in complex biol. mixtures This combined orthogonal strategy permits photocage-selective capture and light-controlled traceless release of target proteins for a myriad of applications in nanoscale assays. After reading the article, we found that the author used 2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate(cas: 76931-93-6Synthetic Route of C8H9NO5S)

2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate(cas: 76931-93-6) belongs to pyrrolidine. Pyrrolidine being a good nucleophile easily undergoes electrophilic substitution reactions with different electrophiles such alkyl halides and acyl halides, and forms N-substituted pyrrolidines. N-Alkylpyrrolidine on further reaction with alkyl halide provided quaternary salts.Synthetic Route of C8H9NO5S

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Tapia, Daniel; Sanchez-Villamil, Javier I.; Torres, Alfredo G. published their research in npj Vaccines on December 31 ,2020. The article was titled 《Multicomponent gold nano-glycoconjugate as a highly immunogenic and protective platform against Burkholderia malleiã€?Quality Control of 2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate The article contains the following contents:

Burkholderia mallei (Bm) is a facultative intracellular pathogen and the etiol. agent of glanders, a highly infectious zoonotic disease occurring in equines and humans. The intrinsic resistance to antibiotics, lack of specific therapy, high mortality, and history as a biothreat agent, prompt the need of a safe and effective vaccine. However, the limited knowledge of protective Bm-specific antigens has hampered the development of a vaccine. Further, the use of antigen-delivery systems that enhance antigen immunogenicity and elicit robust antigen-specific immune responses has been limited and could improve vaccines against Bm. Nanovaccines, in particular gold nanoparticles (AuNPs), have been investigated as a strategy to broaden the repertoire of vaccine-mediated immunity and as a tool to produce multivalent vaccines. To synthesize a nano-glycoconjugate vaccine, six predicted highly immunogenic antigens identified by a genome-wide bio- and immuno-informatic anal. were purified and coupled to AuNPs along with lipopolysaccharide (LPS) from B. thailandensis. Mice immunized intranasally with individual AuNP-protein-LPS conjugates, showed variable degrees of protection against intranasal Bm infection, while an optimized combination formulation (containing protein antigens OmpW, OpcP, and Hemagglutinin, along with LPS) showed complete protection against lethality in a mouse model of inhalational glanders. Animals immunized with different nano-glycoconjugates showed robust antigen-specific antibody responses. Moreover, serum from animals immunized with the optimized nano-glycoconjugate formulation showed sustained antibody responses with increased serum-mediated inhibition of adherence and opsonophagocytic activity in vitro. This study provides the basis for the rational design and construction of a multicomponent vaccine platform against Bm. After reading the article, we found that the author used 2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate(cas: 76931-93-6Quality Control of 2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate)

2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate(cas: 76931-93-6) belongs to pyrrolidine. Pyrrolidine being a good nucleophile easily undergoes electrophilic substitution reactions with different electrophiles such alkyl halides and acyl halides, and forms N-substituted pyrrolidines. N-Alkylpyrrolidine on further reaction with alkyl halide provided quaternary salts.Quality Control of 2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate

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In 2015,Zhai, Tong; Ding, Chunhui; Lu, Lixia; Zhang, Chi; Yang, De’an published 《Autocatalytic deposition of copper coating on poly (ether ether ketone)/multiwalled carbon nanotubes composites via a palladium-free and simplified electroless processã€?Materials Letters published the findings.Category: alcohols-buliding-blocks The information in the text is summarized as follows:

Poly (ether ether ketone)/multiwalled carbon nanotubes composites were metalized by electroless copper plating. The process was based on NaBH4 reducing the Cu2+ ions in electroless plating bath to Cu0 species on the wall of micropores of the swelled composites and simultaneously the Cu0 acted as catalyst initiating the autocatalytic deposition of copper. A dense copper coating was formed. The sheet resistance decreased with increasing the electroless plating time. The adhesion of the copper coating reached the highest 5 B scale according to ASTM D3359. And the electroless process avoided using noble metal Pd as catalyst. In the experiment, the researchers used Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5Category: alcohols-buliding-blocks)

Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5) is a ferroelectric crystal with a high piezoelectric effect and electromechanical coupling coefficient. Category: alcohols-buliding-blocks It is utilized to break up emulsion in organic synthesis as well as a common precipitant in protein crystallography.

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In 2018,Yang, Xing; Cao, Ze-Hun; Zhou, Yang; Cheng, Feng; Lin, Zi-Wei; Ou, Zhi; Yuan, Ye; Huang, Yi-Yong published 《Petasis-Type gem-Difluoroallylation Reactions Assisted by the Neighboring Hydroxyl Group in Aminesã€?Organic Letters published the findings.Related Products of 126456-43-7 The information in the text is summarized as follows:

A three-component Petasis-type gem-difluoroallylation reaction of using pinacol gem-difluoroallylboronates, aldehydes or isatin, and β-amino alcs. enabled by the neighboring hydroxyl group in amine is reported, affording various racemic and chiral gem-difluorohomoallylamine derivatives with good to excellent results. Based on the control experiment and stereochem. of the product, a proposed reaction pathway is illustrated to clarify the origin of regio- and stereoselectivity under protic solvent conditions.(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7Related Products of 126456-43-7) was used in this study.

(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Related Products of 126456-43-7

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In 2018,Cooper, Anna G.; Oyagawa, Caitlin R. M.; Manning, Jamie J.; Singh, Sameek; Hook, Sarah; Grimsey, Natasha L.; Glass, Michelle; Tyndall, Joel D. A.; Vernall, Andrea J. published 《Development of selective, fluorescent cannabinoid type 2 receptor ligands based on a 1,8-naphthyridin-2-(1H)-one-3-carboxamide scaffoldã€?MedChemComm published the findings.Related Products of 27489-62-9 The information in the text is summarized as follows:

Cannabinoid type 2 (CB2) receptor has been implicated in several diseases and conditions, however no CB2 receptor selective drugs have made it to market. The aim of this study was to develop fluorescent ligands as CB2 receptor tools, to enable an increased understanding of CB2 receptor expression and signalling and thereby accelerate drug discovery. Fluorescent ligands have been successfully developed for other receptors, however none with adequate subtype selectivity or imaging properties have been reported for CB2 receptor. A series of 1,8-naphthyridin-2-(1H)-one-3-carboxamides with linkers and fluorophores appended in the N1 and C3-positions were developed. Mol. modeling indicated the C3 cis-cyclohexanol-linked compounds directed the linker out of the CB2 receptor between transmembrane helixes 1 and 7. Herein we report fluorescent ligand 32 (hCB2 pKi = 6.33 ± 0.02) as one of the highest affinity, selective CB2 receptor fluorescent ligands reported. Despite 32 displaying poor specific labeling of CB2 receptor, the naphthyridine scaffold with this linker remains highly promising for future development of CB2 receptor tools. The experimental part of the paper was very detailed, including the reaction process of trans-4-Aminocyclohexanol(cas: 27489-62-9Related Products of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Related Products of 27489-62-9

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