Author: tianli

Heinrich, Timo; Seenisamy, Jeyaprakashnarayanan; Emmanuvel, Lourdusamy; Kulkarni, Santosh S.; Bomke, Joerg; Rohdich, Felix; Greiner, Hartmut; Esdar, Christina; Krier, Mireille; Graedler, Ulrich; Musil, Djordje published the artcile< Fragment-Based Discovery of New Highly Substituted 1H-Pyrrolo[2,3-b]- and 3H-Imidazolo[4,5-b]-Pyridines as Focal Adhesion Kinase Inhibitors>, Name: 2-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, the main research area is pyrrolopyridine imidazolopyridine preparation focal adhesion kinase inhibitor.

Focal adhesion kinase (FAK) is considered as an attractive target for oncol., and small-mol. inhibitors are reported to be in clin. testing. In a surface plasmon resonance (SPR)-mediated fragment screening campaign, we discovered bicyclic scaffolds like 1H-pyrazolo[3,4-d]pyrimidines binding to the hinge region of FAK. By an accelerated knowledge-based fragment growing approach, essential pharmacophores were added. The establishment of highly substituted unprecedented 1H-pyrrolo[2,3-b]pyridine derivatives provided compounds with submicromolar cellular FAK inhibition potential, e.g. I. The combination of substituents on the bicyclic templates and the nature of the core structure itself have a significant impact on the compounds FAK selectivity. Structural anal. revealed that the appropriately substituted pyrrolo[2,3-b]pyridine induced a rare helical DFG-loop conformation. The discovered synthetic route to introduce three different substituents independently paves the way for versatile applications of the 7-azaindole core.

Journal of Medicinal Chemistry published new progress about Drug discovery (fragment-based). 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Name: 2-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Nataraj, Bojan; Maharajan, Kannan; Hemalatha, Devan; Rangasamy, Basuvannan; Arul, Narayanasamy; Ramesh, Mathan published the artcile< Comparative toxicity of UV-filter Octyl methoxycinnamate and its photoproducts on zebrafish development>, HPLC of Formula: 104-76-7, the main research area is toxicity UV Octyl methoxycinnamate photoproduct zebrafish development; Antioxidants; Embryotoxicity; Histopathology; Photoproducts; UV filter; Zebrafish.

In the present study, we explored the adverse effects of Octyl methoxycinnamate (OMC), and its photoproducts, namely 2-ethylhexanol (2-EH) and 4-methoxybenzaldehyde (4-MBA) on the developmental stages of zebrafish using various biomarkers such as developmental toxicity, oxidative stress, antioxidant response, neurotoxicity and histopathol. changes. The 96 h effective concentrations (EC50) of OMC, 2-EH and 4-MBA were found to be 64.0, 34.0 and 3.5μg/mL, resp. in the embryo toxicity test. Embryos exposed to the EC50 of OMC, 2-EH and 4-MBA showed time-dependent increases in the malformation, heart rate and hatching delay. The lipid peroxidation (LPO) level was significantly (p < 0.05) increased and both induction and inhibition of SOD, CAT, GPx and GST activities were observed in the zebrafish embryos exposed to OMC, 2-EH and 4-MBA. GSH activity was significantly (p < 0.05) decreased in the highest exposure groups, when compared with the control. AChE activity was increased in lower concentrations of OMC, 2-EH and 4-MBA exposed embryos whereas, the activity was found to be decreased in highest concentration Moreover, the histopathol. studies showed severe damage to the muscle fibers and yolk sac regions of the larvae with 4-MBA treatment. The photoproduct 4-MBA has the highest toxic effect, followed by 2-EH and OMC. Our results provide useful insights into the impacts of OMC and its photoproducts on zebrafish development. Science of the Total Environment published new progress about Danio rerio. 104-76-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H18O, HPLC of Formula: 104-76-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Schafer, Rebecca J. B.; Monaco, Mattia R.; Li, Mao; Tirla, Alina; Rivera-Fuentes, Pablo; Wennemers, Helma published the artcile< The Bioorthogonal Isonitrile-Chlorooxime Ligation>, Product Details of C6H14ClNO5, the main research area is bioorthogonal isonitrile chlorooxime ligation.

Bioorthogonal reactions are valuable tools for the selective labeling and imaging of natural products and proteins. Here, we present the reaction between isonitriles and chlorooximes as a ligation that proceeds quickly (k ≈ 1 M-1 s-1) and with high chemoselectivity in an aqueous environment. Imaging of metabolically labeled cell surface glycans underlined the tolerance of the ligation to common functional groups in cellular systems. Live-cell dual-labeling experiments revealed that the isonitrile-chlorooxime ligation is orthogonal to the strain-promoted azide-alkyne cycloaddition

Journal of the American Chemical Society published new progress about Azide-alkyne 1,3-dipolar cycloaddition reaction (strain-promoted (SPAAC)). 5505-63-5 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H14ClNO5, Product Details of C6H14ClNO5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Holick, Michael F. published the artcile< Sunlight, UV Radiation, Vitamin D, and Skin Cancer: How Much Sunlight Do We Need?>, Recommanded Product: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, the main research area is vitaminD UV radiation sunlight skin cancer human health; 25-hydroxyvitamin D; Melanoma; Photobiology; Previtamin D; Skin cancer; Sunlight; Ultraviolet radiation; Vitamin D; Vitamin D deficiency; Vitamin D sufficiency.

Vitamin D is the sunshine vitamin for good reason. During exposure to sunlight, the UV B photons enter the skin and photolyze 7-dehydrocholesterol to previtamin D3 which in turn is isomerized by the body′s temperature to vitamin D3. Most humans have depended on sun for their vitamin D requirement. Skin pigment, sunscreen use, aging, time of day, season, and latitude dramatically affect previtamin D3 synthesis. Vitamin D deficiency was thought to have been conquered, but it is now recognized that more than 50% of the world′s population is at risk for vitamin D deficiency. This deficiency is in part due to the inadequate fortification of foods with vitamin D and the misconception that a healthy diet contains an adequate amount of vitamin D. Vitamin D deficiency causes growth retardation and rickets in children and will precipitate and exacerbate osteopenia, osteoporosis and increase risk of fracture in adults. The vitamin D deficiency pandemic has other serious consequences including increased risk of common cancers, autoimmune diseases, infectious diseases, and cardiovascular disease. There needs to be a renewed appreciation of the beneficial effect of moderate sensible sunlight for providing all humans with their vitamin D requirement for health.

Advances in Experimental Medicine and Biology published new progress about Osteopenia. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Recommanded Product: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tamoradi, Taiebeh; Ghorbani-Choghamarani, Arash; Ghadermazi, Mohammad published the artcile< Synthesis of new zirconium complex supported on MCM-41 and its application as an efficient catalyst for synthesis of sulfides and the oxidation of sulfur containing compounds>, Quality Control of 699-12-7, the main research area is sulfide preparation oxidation adenine zirconium nanocatalyst green chem; thiol oxidative coupling adenine zirconium nanocatalyst green chem.

The synthesis of new zirconium complex supported on mesoporous silica by anchoring of adenine on the wall of functionalized MCM-41 and then reacted with ZrOCl2 was described. The resultant MCM-41-Adenine-Zr was characterized by FT-IR, XRD, TEM, SEM, TGA, EDX, ICP and BET techniques. It was exhibited that the MCM-41-Adenine-Zr can be used as an efficient and thermally stable nanocatalyst for the oxidation of sulfides such as dipropylsulfide, tetrahydrothiophene, benzylphenylsulfide, etc.; oxidative coupling of thiols such as naphthalene-2-thiol, benzo[d]thiazole-2-thiol, benzo[d]oxazole-2-thiol, etc. and synthesis of sulfides such as 1,1′-thiobis(2-methoxy)-benzene, 1,1′-thiobis-benzene, 1,1′-thiobis(4-nitro)-benzene. Moreover, this heterogeneous catalyst can be easily recovered from the reaction mixture by simple filtration and reused for several consecutive cycles without noticeable change in its catalytic activity.

Applied Organometallic Chemistry published new progress about Green chemistry. 699-12-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H10OS, Quality Control of 699-12-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zhang, Linlin; Qi, Lin; Chen, Jia-Min; Dong, Wei; Fang, Zhuo-Yue; Cao, Tong-Yang; Li, Wei; Wang, Li-Jing published the artcile< Preparation of selenyl 1,3-oxazines via PhICl2/Cu2O-promoted aminoselenation of O-homoallyl benzimidates with diselenides>, Quality Control of 627-27-0, the main research area is aryl arylselanyl methyl dihydro oxazine preparation; homoallyl benzimidate diselenide aminoselenation catalyst dichloro phenyl iodane copper; oxide.

A practical electrophilic aminoselenation of O-homoallyl benzimidate with diselenides promoted by PhICl2/Cu2O had been developed. The easily available and stable diselenides were used as selenium sources. Various selenyl 1,3-oxazines I [Ar = Ph, 4-MeC6H4, 2-naphthyl, etc.; R1 = H, Me; R2 = H, Ph; R3 = Me, n-Bu, Ph, etc.], which were important frameworks in medicinal and biol. chem., were easily obtained in moderate to good yields for the first time. Easy scaleup and scalability made this method attractive for the preparation of other valuable organoselenides.

Chemical Communications (Cambridge, United Kingdom) published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, Quality Control of 627-27-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kim, Heejin; Kim, Taehoon; Choi, Nakyung; Kim, Byung Hee; Oh, Se-Wook; Kim, In-Hwan published the artcile< Synthesis of diethylhexyl adipate by Candida antarctica lipase-catalyzed esterification>, Electric Literature of 104-76-7, the main research area is diethylhexyl adipate esterification immobilization Candida antarctica lipase.

Diethylhexyl adipate (DEHA) has been used for various applications in the chem. industry. In particular, DEHA is used as a plasticizer for polyvinyl chloride and its polymers. In this study, DEHA was successfully synthesized via lipase-catalyzed esterification from adipic acid with ethylhexanol in a solvent-free system. An immobilized lipase from Candida antarctica (Novozym 435) was used as a biocatalyst in this reaction. The optimal reaction conditions for the synthesis of DEHA were temperature of 50°C, an enzyme loading of 5% (based on the total weight of substrate), a vacuum of 6.7 kPa, and a molar ratio 1:2.5 (adipic acid to ethylhexanol). When vacuum was applied, the conversion to DEHA was improved significantly and 100 mol% conversion was obtained within only 3 h under optimal condition.

Process Biochemistry (Oxford, United Kingdom) published new progress about Optimization. 104-76-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H18O, Electric Literature of 104-76-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Liu, Chao; Song, Liangliang; Peshkov, Vsevolod A.; Van der Eycken, Erik V. published the artcile< Transition metal-free selective C-S bond cleavage of Ugi-adducts for rapid preparation of peptidomimetics>, SDS of cas: 627-27-0, the main research area is peptidomimetic aminal synthesis natural product; Ugi adduct Mannich reaction copper catalyst reaction bond cleavage; Mannich reaction mechanism deprotonation.

A transition metal-free C-S bond cleavage and subsequent Mannich reaction of Ugi-adducts with alcs. as well as thiols is developed. Diverse novel peptidomimetics containing N,O- or N,S-aminals are synthesized in a rapid, highly efficient and step-economical fashion. This method features exclusive selectivity, broad substrate scope, excellent yield and functional group tolerance, and was applied on substrates derived from the pharmaceuticals febuxostat, probenecid and memantine.

Green Chemistry published new progress about Aminals Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, SDS of cas: 627-27-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Li, Xing; Zheng, Leijie; Gong, Xiaolei; Chang, Honghong; Gao, Wenchao; Wei, Wenlong published the artcile< NBS/DBU-Promoted One-Pot Three-Component Cycloaddition of Malonic Acid Derivatives, Nitrosoarenes, and Alkenes: Synthesis of Isoxazolidines>, Synthetic Route of 627-27-0, the main research area is NBS DBU cycloaddition malonic acid nitrosoarene alkene isoxazolidine synthesis.

A general DBU-mediated one-pot three-component cycloaddition reaction of easily accessible malonic acid derivatives, nitrosoarenes, and alkenes has been successfully established with the aid of NBS to provide direct access to highly functionalized isoxazolidine derivatives with generally good to excellent yields, broad functional group tolerance, and excellent regio- and diastereo-selectivities under mild conditions. The mechanism study shows that the NBS-mediated formation of bromomalonic acid derivatives from malonic acid derivatives and DBU-promoted synthesis of nitrone intermediates via the reaction of bromomalonic acid derivatives with nitrosoarenes are key steps.

Journal of Organic Chemistry published new progress about [3+2] Cycloaddition reaction (of nitrone intermediate with olefin, regio- and stereoselective). 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, Synthetic Route of 627-27-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Luo, Huihui; Wang, Lianyue; Shang, Sensen; Li, Guosong; Lv, Ying; Gao, Shuang; Dai, Wen published the artcile< Cobalt Nanoparticles-Catalyzed Widely Applicable Successive C-C Bond Cleavage in Alcohols to Access Esters>, COA of Formula: C8H9FO, the main research area is ester preparation cobalt nanoparticle catalyst carbon bond cleavage alc; C−C bond; aerobic oxidative cleavage; alcohols; esters; heterogeneous cobalt catalyst.

Selective cleavage and functionalization of C-C bonds have important applications in organic synthesis and biomass use. However, functionalization of C-C bonds by controlled cleavage remains difficult and challenging because they are inert. Herein, the authors describe an unprecedented efficient protocol for the breaking of successive C-C bonds in alcs. to form esters with one or multiple carbon atoms less using heterogeneous cobalt nanoparticles as catalyst with dioxygen as the oxidant. A wide range of alcs. including inactive long-chain alkyl aryl alcs. undergo smoothly successive cleavage of adjacent -(C-C)n- bonds to afford the corresponding esters. The catalyst was used for seven times without any decrease in activity. Characterization and control experiments disclose that cobalt nanoparticles are responsible for the successive cleavage of C-C bonds to achieve excellent catalytic activity, while the presence of Co-Nx has just the opposite effect. Preliminary mechanistic studies reveal that a tandem sequence reaction is involved in this process.

Angewandte Chemie, International Edition published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 403-41-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H9FO, COA of Formula: C8H9FO.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts