Tag: 100-200

Park, Kwihwan; Jiang, Jing; Yamada, Tsuyoshi; Sajiki, Hironao published their research in Chemical & Pharmaceutical Bulletin in 2021. The article was titled 《Ruthenium-on-carbon-catalyzed facile solvent-free oxidation of alcohols: efficient progress under solid-solid (liquid)-gas conditions》.Recommanded Product: 3-Pyridinemethanol The article contains the following contents:

A protocol for the ruthenium-on-carbon (Ru/C)-catalyzed solvent-free oxidation of alcs., which proceeds efficiently under solid-solid (liquid)-gas conditions, was developed. Various primary and secondary alcs. were transformed to corresponding aldehydes and ketones in moderate to excellent isolated yields by simply stirring in the presence of 10% Ru/C under air or oxygen conditions. The solvent-free oxidation reactions proceeded efficiently regardless of the solid or liquid state of the substrates and reagents and could be applied to gram-scale synthesis without loss of the reaction efficiency. Furthermore, the catalytic activity of Ru/C was maintained after five reuse cycles. In addition to this study using 3-Pyridinemethanol, there are many other studies that have used 3-Pyridinemethanol(cas: 100-55-0Recommanded Product: 3-Pyridinemethanol) was used in this study.

3-Pyridinemethanol(cas: 100-55-0) belongs to pyridine. Pyridine is widely used in the precursor to agrochemicals and pharmaceuticals. Also, it is used as an important reagent and organic solvent.Recommanded Product: 3-Pyridinemethanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Synthesis, characterization, DNA/BSA interactions and in vitro cytotoxicity study of palladium(II) complexes of hispolon derivatives》 was published in Journal of Inorganic Biochemistry in 2020. These research results belong to Wei, Xiaonan; Yang, Yaxing; Ge, Jiangfeng; Lin, Xue; Liu, Dandan; Wang, Shuxiang; Zhang, Jinchao; Zhou, Guoqiang; Li, Shenghui. Related Products of 26153-38-8 The article mentions the following:

Thirteen novel palladium(II) complexes of the general formula [Pd(bipy)(O,O’-dkt)](PF6), (where bipy is 2,2′-bipyridine and O,O’-dkt is β-diketonate ligand hispolon or its derivative) have been prepared through a metal-ligand coordination method that involves spontaneous formation of the corresponding diketonate scaffold. The obtained palladium(II) complexes have been characterized by NMR spectroscopy, ESI-mass spectrometry as well as elemental anal. The cytotoxicity anal. indicates that most of the obtained palladium(II) complexes show promising growth inhibition in three human cancer cell lines. Flow cytometry anal. shows complex 3e could promote intracellular reactive oxygen species (ROS) accumulation and lead cancer cell death. And the suppression of ROS accumulation and the rescue of cell viability in HeLa cells by N-acetyl-L-cysteine (NAC) suggest the possible link between the increase in ROS generation and cytotoxicity of complex 3e. Flow cytometry anal. also reveal that complex 3e cause cell cycle arrest in the G2/M phase and collapse of the mitochondrial membrane potential, promote the generation of ROS and lead to tumor cell apoptosis. The interactions of complex 3e with calf thymus DNA (CT-DNA) have been evaluated by UV-Vis spectroscopy, fluorescence quenching experiments and viscosity measurements, which reveal that the complex interact with CT-DNA through minor groove binding and/or electrostatic interactions. Further, the results of fluorescence titration and site marker competitive experiment on bovine serum albumin (BSA) suggest that complex 3e can quench the fluorescence of BSA via a static quenching process and bind to BSA in Sudlow’s site II. In addition to this study using 3,5-Dihydroxybenzaldehyde, there are many other studies that have used 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Related Products of 26153-38-8) was used in this study.

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is used as a building block in the synthesis of more complex structures. It is also used in the synthesis of terbutaline, which is an important bronchodilator.Related Products of 26153-38-8

Referemce:
Alcohol – Wikipedia,
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《Synthesis, biological evaluation and molecular docking study of dihydropyrimidine derivatives as potential anticancer agents》 was published in Journal of Heterocyclic Chemistry in 2020. These research results belong to Safari, Sahand; Ghavimi, Reza; Razzaghi-Asl, Nima; Sepehri, Saghi. Application of 100-83-4 The article mentions the following:

A series of dihydropyrimidine analogs I (R = H, 3-Cl, 2-OH, 4-NO2, etc.; R1 = Et, Ph; X = O, S) was prepared via one-pot Biginelli three-component condensation reaction. Subsequently, they were screened for in vitro anticancer effect. These analogs revealed good cytotoxic activity against three human cancer cell lines including MCF-7, HepG-2, and A549. Among these analogs, compounds I (R = H, R1 = Ph, X = S (A); R = 4-NO2, R1 = Ph, X = S (B)) were the most potent against three cell lines. Cell viability assays indicated that I (R = H, R1 = Ph, X = O; R = 2-OH, R1 = Ph, X = O) had lower cytotoxicity. In vitro cytotoxicity study on all synthesized compounds demonstrated that introduction of electron withdrawing substituents on C4 position of Ph ring of dihydropyrimidine contributed to the antiproliferative potency. Moreover, in silico mol. docking results stipulated a sign of good correlation between exptl. activity and calculated binding affinity. It proved (A) and (B) as the strongest compounds Binding modes of analogs proposed the involvement of hydrophobic interactions and hydrogen bonds with Eg5 active site. Structure activity relationship studies indicated that incorporating electron withdrawing substituents on C4 position of Ph ring of dihydropyrimidine are important for this biol. activity. After reading the article, we found that the author used 3-Hydroxybenzaldehyde(cas: 100-83-4Application of 100-83-4)

3-Hydroxybenzaldehyde(cas: 100-83-4) can be used as a reactant along with ethyl acetoacetate and thiourea in the synthesis of corresponding dihydropyrimidine-2-thione (monastrol), using Yb(OTf)3 as a catalyst by Biginelli cyclocondensation reaction.Application of 100-83-4

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《Organophotoredox-Mediated Amide Synthesis by Coupling Alcohol and Amine through Aerobic Oxidation of Alcohol》 was published in Chemistry – A European Journal in 2020. These research results belong to Shah, Sk. Sheriff; Shee, Maniklal; Venkatesh, Yarra; Singh, Amit Kumar; Samanta, Samya; Singh, N. D. Pradeep. COA of Formula: C7H7BrO The article mentions the following:

The combination of an organic photocatalyst [4CzIPN (1,2,3,5-tetrakis(carbazol-9-yl)-4,6-dicyanobenzene) or 5MeOCzBN (2,3,4,5,6-pentakis(3,6-dimethoxy-9 H-carbazol-9-yl)benzonitrile)], quinuclidine, and tetra-n-butylammonium phosphate (hydrogen-bonding catalyst) was employed for amide bond formations. The hydrogen-bonded OH group activated the adjacent C-H bond of alcs. towards hydrogen atom transfer (HAT) by a radical species. The quinuclidinium radical cation, generated through single-electron oxidation of quinuclidine by the photocatalyst, employed to abstract a hydrogen atom from the α-C-H bond of alcs. selectively due to a polarity effect-produced α-hydroxyalkyl radical, which subsequently converted to the corresponding aldehyde under aerobic conditions. Then the coupling of the aldehyde and an amine formed a hemiaminal intermediate that upon photocatalytic oxidation produced the amide. In the part of experimental materials, we found many familiar compounds, such as (4-Bromophenyl)methanol(cas: 873-75-6COA of Formula: C7H7BrO)

(4-Bromophenyl)methanol(cas: 873-75-6) undergoes three-component reaction with acetylferrocene and arylboronic acid to give ferrocenyl ketones containing biaryls.COA of Formula: C7H7BrO It undergoes oxidation reaction in the presence of polyvinylpolypyrrolidone-supported hydrogen peroxide, silica sulfuric acid and ammonium bromide to yield 4-bromobenzaldehyde.

Referemce:
Alcohol – Wikipedia,
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In 2019,ACS Applied Materials & Interfaces included an article by Ding, Jiheng; Zhao, Hongran; Shao, Zhenzong; Yu, Haibin. Recommanded Product: 6-Aminohexan-1-ol. The article was titled 《Bioinspired Smart Anticorrosive Coatings with an Emergency-Response Closing Function》. The information in the text is summarized as follows:

Emergency-response closing (ERC) of diffusion pathways for aggressive species in graphene/epoxy (G/EP) coatings was achieved via terpyridine derivative (TDD)-functionalized graphene oxide (tGO). Under stimulation from corrosion produced ferrous (Fe2+) ions, tGO sheets urgently aggregated through complexation reminiscent of leaves closing on a mimosa. Consequently, the coating showed significantly decreased oxygen (ORT) and water vapor transmittance rate (WVTR) changes after immersion in ferrous solution According to the simulation and electrochem. results, tGO sheets could self-assemble into 3D architectures with Fe2+ ions and efficiently protect metals from aggressive species attack. This tGO/EP coating provided an ERC function via self-adaptability with the Fe2+ ions to achieve long-term anticorrosion. The application of tGO/EP to the protection of metal components is therefore validated as a fascinating route for the enhancement of anticorrosion efficiency on graphene anticorrosive coatings, with great potential in durable anticorrosive coatings application. The results came from multiple reactions, including the reaction of 6-Aminohexan-1-ol(cas: 4048-33-3Recommanded Product: 6-Aminohexan-1-ol)

6-Aminohexan-1-ol(cas: 4048-33-3) may be used along with glutaric acid to generate poly(ester amide)s with excellent film- and fiber forming properties. It can undergo cyclization over copper supported on γ-alumina and magnesia to form hexahydro-1H-azepine.Recommanded Product: 6-Aminohexan-1-ol

Referemce:
Alcohol – Wikipedia,
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In 2018,Nitha, P. R.; Joseph, Manu M.; Gopalan, Greeshma; Maiti, Kaustabh Kumar; Radhakrishnan, K. V.; Das, Parthasarathi published 《Chloroform as a carbon monoxide source in palladium-catalyzed synthesis of 2-amidoimidazo[1,2-a]pyridines》.Organic & Biomolecular Chemistry published the findings.Name: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol The information in the text is summarized as follows:

A palladium-catalyzed aminocarbonylation strategy exploiting chloroform as a CO source has been developed for the synthesis of biol. potent 2-amidoimidazopyridine I (R1, R2 = -(CH2)4-, -(CH2)5-, cyclohexyl, etc.) scaffolds. The aminocarbonylation reaction was found to be general with a range of amines and substituted imidazopyridines. Preliminary biol. evaluation of cytotoxicity on selected examples provides scope for future investigations. In the part of experimental materials, we found many familiar compounds, such as (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7Name: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol)

(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Name: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol

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In 1996,Dave, Paritosh R. published 《Acylative Dealkylation of N-tert-Butyl-3-substituted Azetidines: Facile Access to [1.1.0]Azabicyclobutane, 3-Hydroxyazetidinium Hydrochloride, and 3-Azetidinones》.Journal of Organic Chemistry published the findings.Safety of Azetidin-3-ol hydrochloride The information in the text is summarized as follows:

A novel acylative dealkylation of N-tert-butylazetidines and its application to the facile high-yield syntheses of [1.1.0]azabicyclobutane, 3-hydroxyazetidinium hydrochloride, and 3-azetidinones is described. In the experiment, the researchers used many compounds, for example, Azetidin-3-ol hydrochloride(cas: 18621-18-6Safety of Azetidin-3-ol hydrochloride)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Safety of Azetidin-3-ol hydrochloride Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
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The author of 《2-[(Phenylthio)methyl]pyridine derivatives: new antiinflammatory agents》 were Haviv, Fortuna; DeNet, Robert W.; Michaels, Raymond J.; Ratajczyk, James D.; Carter, George W.; Young, Patrick R.. And the article was published in Journal of Medicinal Chemistry in 1983. Application of 55218-73-0 The author mentioned the following in the article:

The title compounds I (R = H, Br, Cl, F, Me, NH2, OMe, etc., R1 = H, Cl, OH, Me, OMe, Ph, etc.) and related compounds as the HCl salts, prepared mostly by the reaction of 2-picolyl chloride [4377-33-7] or 2-(hydroxymethyl)pyridine  [586-98-1] with the appropriate mercaptol either in 48% HBr under reflux or in the presence of NaOEt in EtOH at room temperature, were investigated as inflammation inhibitors in rat. I (R = H, Br, Cl, F, or NO2 and R1 = H) were effective inhibitors of immune complex induced inflammation as represented by the rat reverse passive Arthus reaction. 2-[[(4-bromophenyl)thio]methyl]pyridine (I; R = Br, R1 = H) [83782-10-9] also inhibited both exudate formation and cellular accumulation in the more conventional carrageenin pleural test, whereas indomethacin inhibited only exudate volume in this model. Structure-activity relations are discussed. The results came from multiple reactions, including the reaction of (4-Phenylpyridin-2-yl)methanol(cas: 55218-73-0Application of 55218-73-0)

(4-Phenylpyridin-2-yl)methanol(cas: 55218-73-0) belongs to hydroxy-containing compounds. Hydroxy groups participate in the dehydration reactions that link simple biological molecules into long chains. The creation of a peptide bond to link two amino acids to make a protein removes the −OH from the carboxy group of one amino acid.Application of 55218-73-0

Referemce:
Alcohol – Wikipedia,
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Synthetic Route of C6H13NOIn 2018 ,《Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent》 was published in Bioorganic & Medicinal Chemistry. The article was written by Xiang, Weiguo; Choudhary, Shruti; Hamel, Ernest; Mooberry, Susan L.; Gangjee, Aleem. The article contains the following contents:

We report a series of tubulin targeting agents, some of which demonstrate potent antiproliferative activities. These analogs were designed to optimize the antiproliferative activity of 1 by varying the heteroatom substituent at the 4′-position, the basicity of the 4-position amino moiety, and conformational restriction. The potential metabolites of the active compounds were also synthesized. Some compounds demonstrated single digit nanomolar IC50 values for antiproliferative effects in MDA-MB-435 melanoma cells. Particularly, the S-Me analog 3 was more potent than 1 in MDA-MB-435 cells (IC50 = 4.6 nM). Incubation of 3 with human liver microsomes showed that the primary metabolite of the S-Me moiety of 3 was the Me sulfinyl group, as in analog 5. This metabolite was equipotent with the lead compound 1 in MDA-MB-435 cells (IC50 = 7.9 nM). Mol. modeling and electrostatic surface area were determined to explain the activities of the analogs. Most of the potent compounds overcome multiple mechanisms of drug resistance and compound 3 emerged as the lead compound for further SAR and preclin. development. The results came from multiple reactions, including the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Synthetic Route of C6H13NO)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Synthetic Route of C6H13NO

Referemce:
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Quality Control of trans-4-AminocyclohexanolIn 2017 ,《Discovery of 4-((3’R,4’S,5’R)-6”-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2”-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3”-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development》 was published in Journal of Medicinal Chemistry. The article was written by Aguilar, Angelo; Lu, Jianfeng; Liu, Liu; Du, Ding; Bernard, Denzil; McEachern, Donna; Przybranowski, Sally; Li, Xiaoqin; Luo, Ruijuan; Wen, Bo; Sun, Duxin; Wang, Hengbang; Wen, Jianfeng; Wang, Guangfeng; Zhai, Yifan; Guo, Ming; Yang, Dajun; Wang, Shaomeng. The article contains the following contents:

The authors previously reported the design of spirooxindoles with two identical substituents at the carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this paper the authors describe an extensive structure-activity relationship study of this class of MDM2 inhibitors, which led to the discovery of 60 (AA-115/APG-115, 4-((3R,4S,5R)-6”-chloro-4-(3-chloro-2-fluorophenyl)-1-ethyl-2”-oxodispiro[cyclohexane-1,2-pyrrolidine-3,3”-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic acid). Compound 60 has a very high affinity to MDM2 (Ki < 1 nM), potent cellular activity, and an excellent oral pharmacokinetic profile. Compound 60 is capable of achieving complete and long-lasting tumor regression in vivo and is currently in phase I clin. trials for cancer treatment. In addition to this study using trans-4-Aminocyclohexanol, there are many other studies that have used trans-4-Aminocyclohexanol(cas: 27489-62-9Quality Control of trans-4-Aminocyclohexanol) was used in this study.

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Quality Control of trans-4-Aminocyclohexanol

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