Category: 209919-30-2

Feofanov, Mikhail published the artcileSolid-state construction of zigzag periphery via intramolecular C-H insertion induced by alumina-mediated C-F activation, Application of 4-Chloro-2-methylphenylboronic acid, the publication is Chemical Communications (Cambridge, United Kingdom) (2021), 57(92), 12325-12328, database is CAplus and MEDLINE.

Here, the alumina-mediated C-F bond activation (AmCFA) enabled construction of PAHs with zigzag periphery was reported. This method includes formal Csp³-H activation and opens an avenue for generation of carbon-based nanomagnets directly on technol. relevant surfaces.

Chemical Communications (Cambridge, United Kingdom) published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Application of 4-Chloro-2-methylphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Cross, R. Matthew published the artcileOrally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is Journal of Medicinal Chemistry (2014), 57(21), 8860-8879, database is CAplus and MEDLINE.

The continued proliferation of malaria throughout temperate and tropical regions of the world has promoted a push for more efficacious treatments to combat the disease. Unfortunately, more recent remedies such as artemisinin combination therapies have been rendered less effective due to developing parasite resistance, and new drugs are required that target the parasite in the liver to support the disease elimination efforts. Research was initiated to revisit antimalarials developed in the 1940s and 1960s that were deemed unsuitable for use as therapeutic agents as a result of poor understanding of both physicochem. properties and parasitol. Structure-activity and structure-property relationship studies were conducted to generate a set of compounds with the general 6-chloro-7-methoxy-2-methyl-4(1H)-quinolone scaffold which were substituted at the 3-position with a variety of Ph moieties possessing various properties. Extensive physicochem. evaluation of the quinolone series was carried out to down-select the most promising 4(1H)-quinolones, P4Q-391 (7), 6-Chloro-7-methoxy-2-methyl-3-(2-methyl-4-(4(trifluoromethoxy)phenoxy)phenyl)-quinolin-4(1H)-one (62), 6-Chloro-3-(6-(2-fluoro-4-(trifluoromethyl)phenyl)pyridin-3-yl)-7-methoxy-2-methylquinolin-4(1H)-one (66), and 6-Chloro-7-methoxy-2-methyl-3-(6-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)quinolin-4(1H)-one(67), which possessed low-nanomolar EC₅₀ values against W2 and TM90-C2B as well as improved microsomal stability. Addnl., in vivo Thompson test results using Plasmodium berghei in mice showed that these 4(1H)-quinolones were efficacious for the reduction of parasitemia at >99% after 6 days.

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Bouton, Jakob published the artcileRevisiting Pyrazolo[3,4-d]pyrimidine Nucleosides as Anti-Trypanosoma cruzi and Antileishmanial Agents, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is Journal of Medicinal Chemistry (2021), 64(7), 4206-4238, database is CAplus and MEDLINE.

Chagas disease and visceral leishmaniasis are two neglected tropical diseases responsible for numerous deaths around the world. For both, current treatments are largely inadequate, resulting in a continued need for new drug discovery. As both kinetoplastid parasites are incapable of de novo purine synthesis, they depend on purine salvage pathways that allow them to acquire and process purines from the host to meet their demands. Purine nucleoside analogs therefore constitute a logical source of potential antiparasitic agents. Earlier optimization efforts of the natural product tubercidin (7-deazaadenosine) involving modifications to the nucleobase 7-position and the ribofuranose 3′-position led to analogs with potent anti-Trypanosoma brucei and anti-Trypanosoma cruzi activities. In this work, we report the design and synthesis of pyrazolo[3,4-d]pyrimidine nucleosides with 3′- and 7-modifications and assess their potential as anti-Trypanosoma cruzi and antileishmanial agents. One compound was selected for in vivo evaluation in an acute Chagas disease mouse model.

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Li, Jia published the artcileDiscovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists, Related Products of chlorides-buliding-blocks, the publication is Chemical Biology & Drug Design (2018), 92(1), 1241-1254, database is CAplus and MEDLINE.

A novel series of thiophene-containing biaryl amide derivatives I (R¹ = 4-FC₆H₄, 4-CF₃OC₆H₄, 4-t-BuC₆H₄, etc.; R² = 2-Me-4-ClC₆H₃, 3-Me-4-ClC₆H₃, 2,4,6-(Me)₃) as glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, I (R¹ = 4-CF₃OC₆H₄; R² = 2-Me-4-ClC₆H₃) and I (R¹ = 4-t-BuC₆H₄; R² = 2-Me-4-ClC₆H₃), exhibited good GCGR binding (IC₅₀ = 6.1 and 4.4 μM, resp.) and cAMP functional activities (IC₅₀ = 4.4 and 14.4 μM, resp.). The possible binding modes of above two compounds with GCGR were explored by mol. simulation.

Chemical Biology & Drug Design published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Zhang, Jitan published the artcilePalladium-catalyzed Atroposelective Interannular C-H Arylation of Biaryl Aldehydes with Aryl Iodides Enabled by a Transient Directing Group Strategy, Application of 4-Chloro-2-methylphenylboronic acid, the publication is Advanced Synthesis & Catalysis (2022), 364(20), 3589-3599, database is CAplus.

A concise synthesis of axially chiral biaryl aldehydes through Pd/amino acid-catalyzed atroposelective interannular C-H arylation of biaryl aldehydes with aryl iodides is developed. This reaction proceeds smoothly involving excellent enantiocontrol and accomplishes with good tolerance of functional groups. Moreover, the readily accessible scale-up synthesis and further transformation of products has highlighted the potential utility of this asym. catalytic protocol.

Advanced Synthesis & Catalysis published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C20H17FO4S, Application of 4-Chloro-2-methylphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Khalaf, Juhienah published the artcileDesign, Synthesis, and Diversification of 3,5-Substituted Enone Library, SDS of cas: 209919-30-2, the publication is ACS Combinatorial Science (2011), 13(4), 351-356, database is CAplus and MEDLINE.

This paper describes the synthesis of a 300 member library of 3,5-substituted enones, e.g., I. The synthesis starts with six different bromoenones that are accessed from the corresponding 1,3 diones. These bromides are then diversified by Suzuki coupling with a variety of aromatic and vinyl boronic acids. Addnl. a small series of triazoles, e.g., II, were synthesized by a Sonogashira coupling reaction dipolar cycloaddition sequence. The library was analyzed by principal component anal. to examine its diversity.

ACS Combinatorial Science published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, SDS of cas: 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Yoon, Taeyoung published the artcileThe design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists, Application In Synthesis of 209919-30-2, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(3), 891-896, database is CAplus and MEDLINE.

The design, synthesis and structure-activity relationships of a series of CRF-1 receptor antagonist, the 1-aryl-4-alkylaminoisoquinolines, is described. The effects of substitution on the aromatic ring, the amino group and the isoquinoline core on CRF-1 receptor binding were investigated.

Bioorganic & Medicinal Chemistry Letters published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C2H5BF3K, Application In Synthesis of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Wu, Qian published the artcileUnified synthesis of mono/bis-arylated phenols via Rh^III-catalyzed dehydrogenative coupling, Application In Synthesis of 209919-30-2, the publication is Chemical Science (2017), 8(1), 169-173, database is CAplus and MEDLINE.

A general strategy that allowed for the precise control of the oxidation pathways so that directing groups can be either preserved or cleaved was reported. It was found that N-phenoxyacetamides underwent ortho-arylation reactions with or without an external oxidant, yielding products with different oxidation states, notably the rare bis-arylated phenols. Notably, a unique rhodacycle intermediate was isolated, characterized by X-ray crystallog. and confirmed to be an active catalyst. Switching between internal and external oxidation could be a general strategy in diverse directed C-H functionalization reactions to realize bis-functionalized products.

Chemical Science published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C11H8O3, Application In Synthesis of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Lumeras, Wenceslao published the artcileDesign, Synthesis, and Structure-Activity Relationships of Aminopyridine N-Oxides, a Novel Scaffold for the Potent and Selective Inhibition of p38 Mitogen Activated Protein Kinase, Synthetic Route of 209919-30-2, the publication is Journal of Medicinal Chemistry (2009), 52(17), 5531-5545, database is CAplus and MEDLINE.

A novel series of aminopyridine N-oxides, e.g. I, were designed, synthesized, and tested for their ability to inhibit p38α MAP kinase. Some of these compounds showed a significant reduction in the LPS-induced TNFα production in human whole blood. Structure-activity relationship studies revealed that N-oxide oxygen was essential for activity and was probably a determinant factor for a marked selectivity against other related kinases. Compound I was identified as a potent and selective p38α inhibitor with an appropriate balance between potency and pharmacokinetics. In vivo efficacy of I was demonstrated in reducing TNFα levels in an acute murine model of inflammation (ED₅₀ = 1 mg/kg in LPS-induced TNFα production when dosed orally 1.5 h prior to LPS administration). The oral efficacy of I was further demonstrated in a chronic model of adjuvant arthritis in rats with established disease when administered orally (ED₅₀ = 4.5 mg/kg).

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Synthetic Route of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics