Category: 480438-56-0

Laha, Joydev K. published the artcileScope of Successive C-H Functionalizations of the Methyl Group in 3-Picolines: Intramolecular Carbonylation of Arenes to the Metal-Free Synthesis of 4-Azafluorenones, HPLC of Formula: 480438-56-0, the publication is Organic Letters (2015), 17(23), 5890-5893, database is CAplus and MEDLINE.

A transition-metal-free, t-BuOOH mediated intramol. carbonylation of arenes in 2-aryl-3-picolines via oxidative C-H functionalizations of the Me group has been developed, providing an expedient synthesis of 4-azafluorenones I [R = 7-MeO, 7-OCF₃, 6,7-Cl₂, 6-Cl-7-OPr-i, 7,8-(OMe)₂, etc] . Distinct from the current literature wherein methylarenes have been used as acylating agents, 2-aryl-3-picolines in this study are transformed into aldehydes, which give 4-azafluorenones upon rapid intramol. acylation. The study demonstrates the first example of intramol. carbonylation of arenes utilizing a Me group as latent carbonyl functionality.

Organic Letters published new progress about 480438-56-0. 480438-56-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, HPLC of Formula: 480438-56-0.

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

Seth, Kapileswar published the artcile2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation, Formula: C9H12BClO3, the publication is ACS Medicinal Chemistry Letters (2014), 5(5), 512-516, database is CAplus and MEDLINE.

The 2-(2-arylphenyl)benzoxazole moiety has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The 2-(2-arylphenyl)benzoxazoles I [R = (un)substituted Ph] have been synthesized by Suzuki reaction of 2-(2-bromophenyl)benzoxazole. The compounds II, III, and IV selectively inhibited COX-2 with selectivity index of III much better than that of the COX-2 selective NSAID celecoxib. The in vivo anti-inflammatory potency of II and III is comparable to that of celecoxib and the nonselective NSAID diclofenac at two different doses, and IV showed better potency compared to these clin. used NSAIDs.

ACS Medicinal Chemistry Letters published new progress about 480438-56-0. 480438-56-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C13H10O2, Formula: C9H12BClO3.

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

Fujiwara, Yuta published the artcilePractical C-H Functionalization of Quinones with Boronic Acids, Product Details of C9H12BClO3, the publication is Journal of the American Chemical Society (2011), 133(10), 3292-3295, database is CAplus and MEDLINE.

A direct functionalization of a variety of quinones with several boronic acids has been developed. This scalable reaction proceeds readily at room temperature in an open flask using catalytic silver(I) nitrate in the presence of a persulfate co-oxidant. The scope with respect to quinones is broad, with a variety of alkyl- and arylboronic acids undergoing efficient cross-coupling. The mechanism is presumed to proceed through a nucleophilic radical addition to the quinone with in situ reoxidation of the resulting dihydroquinone. This method has been applied to complex substrates, including a steroid derivative and a farnesyl natural product.

Journal of the American Chemical Society published new progress about 480438-56-0. 480438-56-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Product Details of C9H12BClO3.

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

Yu, Haihua published the artcileControllable access to multi-substituted imidazoles via palladium(II)-catalyzed C-C coupling and C-N condensation cascade reactions, HPLC of Formula: 480438-56-0, the main research area is imidazole preparation; aminoacetonitrile boronic acid palladium catalyst cascade condensation cyclization.

A novel and efficient protocol for the synthesis of various 2,4-disubstituted, 1,2,4-trisubstituted and 1,2,4,5-tetra-substituted imidazoles I [R1 = Me, CF3, Ph, etc.; R2 = H, Ph, Bn; R3 = H, Me; R4 = Ph, 4-FC6H4, 2-MeC6H4, etc.] via cascade palladium catalyzed C-C coupling followed by intramol. C-N bond formation was developed. Readily accessible boronic acids and N-substituted-2-aminoacetonitriles were firstly reported as starting materials to construct di-, tri-, and tetra-substituted imidazoles in good to excellent yield. The protocol was the first report to prepare multi-substituted imidazoles from readily accessible aminoacetonitrile and boronic acid.

Chemical Communications (Cambridge, United Kingdom) published new progress about Condensation reaction. 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, HPLC of Formula: 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Seth, Kapileswar published the artcile2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation, Synthetic Route of 480438-56-0, the main research area is arylphenylbenzoxazole preparation cyclooxygenase2 inhibitor; antiinflammatory arylphenylbenzoxazole preparation; benzoxazole arylphenyl preparation cyclooxygenase2 inhibitor; 2-(2-Arylphenyl)benzoxazoles; 3D QSAR; cyclooxygenase-2 selective; in vivo potency; novel anti-inflammatory scaffold.

The 2-(2-arylphenyl)benzoxazole moiety has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The 2-(2-arylphenyl)benzoxazoles I [R = (un)substituted Ph] have been synthesized by Suzuki reaction of 2-(2-bromophenyl)benzoxazole. The compounds II, III, and IV selectively inhibited COX-2 with selectivity index of III much better than that of the COX-2 selective NSAID celecoxib. The in vivo anti-inflammatory potency of II and III is comparable to that of celecoxib and the nonselective NSAID diclofenac at two different doses, and IV showed better potency compared to these clin. used NSAIDs.

ACS Medicinal Chemistry Letters published new progress about Cyclooxygenase 2 inhibitors. 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Synthetic Route of 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Toledo-Sherman, Leticia M. published the artcileDevelopment of a Series of Aryl Pyrimidine Kynurenine Monooxygenase Inhibitors as Potential Therapeutic Agents for the Treatment of Huntington’s Disease, Computed Properties of 480438-56-0, the main research area is arylpyrimidine kynurenine monooxygenase inhibitor preparation SAR Huntingtons disease.

We report on the development of a series of pyrimidine carboxylic acids that are potent and selective inhibitors of kynurenine monooxygenase and competitive for kynurenine. We describe the SAR for this novel series and report on their inhibition of KMO activity in biochem. and cellular assays and their selectivity against other kynurenine pathway enzymes. We describe the optimization process that led to the identification of a program lead compound with a suitable ADME/PK profile for therapeutic development. We demonstrate that systemic inhibition of KMO in vivo with this lead compound provides pharmacodynamic evidence for modulation of kynurenine pathway metabolites both in the periphery and in the central nervous system.

Journal of Medicinal Chemistry published new progress about Central nervous system agents. 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Computed Properties of 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Laha, Joydev K. published the artcileScope of Successive C-H Functionalizations of the Methyl Group in 3-Picolines: Intramolecular Carbonylation of Arenes to the Metal-Free Synthesis of 4-Azafluorenones, HPLC of Formula: 480438-56-0, the main research area is picoline aryl oxidant intramol carbonylation; azafluorenone preparation.

A transition-metal-free, t-BuOOH mediated intramol. carbonylation of arenes in 2-aryl-3-picolines via oxidative C-H functionalizations of the Me group has been developed, providing an expedient synthesis of 4-azafluorenones I [R = 7-MeO, 7-OCF3, 6,7-Cl2, 6-Cl-7-OPr-i, 7,8-(OMe)2, etc] . Distinct from the current literature wherein methylarenes have been used as acylating agents, 2-aryl-3-picolines in this study are transformed into aldehydes, which give 4-azafluorenones upon rapid intramol. acylation. The study demonstrates the first example of intramol. carbonylation of arenes utilizing a Me group as latent carbonyl functionality.

Organic Letters published new progress about C-H bond activation (oxidative). 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, HPLC of Formula: 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gourdet, Benoit published the artcileRhodium-catalyzed carbometalation of ynamides with organoboron reagents, Quality Control of 480438-56-0, the main research area is oxazolidinone alkynyl rhodium catalyst carbometalation; ynamide carbometalation stereoselective regioselective rhodium catalyst; enamide stereoselective regioselective preparation.

In the presence of catalytic [Rh(cod)(MeCN)2]BF4, ynamides undergo carbometalation with boronic acids, arylboronic esters, and triarylboroxines. These reactions enable the regio- and stereocontrolled synthesis of multisubstituted enamides. E.g., reaction of 3-(2-phenylethynyl)oxazolidin-2-one with 4-chlorophenylboronic acid gave 65% 3-[(E)-2-(4-chlorophenyl)-2-phenylvinyl]oxazolidin-2-one (I).

Tetrahedron published new progress about Addition reaction catalysts, regioselective. 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Quality Control of 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Bernardo, Paul H. published the artcileSynthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1, Computed Properties of 480438-56-0, the main research area is mol docking anticancer agent rhodanine pyridine amino acid preparation.

Symposium report presented at the 18th International Conference on Organic Synthesis (ICOS) Bergen, Norway 1-6 August, 2010. A small library of pyridine-based rhodanine analogs of BH-3I-1 [i.e., 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-3-thiazolidineacetic acid] was designed, the synthesis of the target compound was achieved using amino acids as starting materials and the products thus obtained were screened against B-cell lymphoma (extra large, Bcl-XL, antiapoptotic protein, inhibitor of apoptosis proteins) and myeloid cell leukemia sequence 1 (Mcl-1) for the ability to displace 5-(carboxy)fluorescein-labeled Bak peptide (Flu-Bak). Differences in selectivity toward Bcl-XL and Mcl-1 were observed and the binding modes of selected compounds were studied further. The results may be useful in designing potent small-mol. inhibitors of Bcl-XL and Mcl-1 as well as selective Mcl-1 inhibitors.

Pure and Applied Chemistry published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Computed Properties of 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yap, Connor published the artcileEnantioselective Nickel-Catalyzed Intramolecular Allylic Alkenylations Enabled by Reversible Alkenylnickel E/Z Isomerization, Product Details of C9H12BClO3, the main research area is alkynylallylic phosphate arylboronic acid nickel enantioselective allylic alkenylation isomerization; allylic substitution; asymmetric catalysis; cyclization; isomerization; nickel.

Enantioselective nickel-catalyzed arylative cyclizations of substrates containing a Z-allylic phosphate tethered to an alkyne are described. These reactions give multisubstituted chiral aza- and carbocycles, and are initiated by the addition of an arylboronic acid to the alkyne, followed by cyclization of the resulting alkenylnickel species onto the allylic phosphate. The reversible E/Z isomerization of the alkenylnickel species is essential for the success of the reactions.

Angewandte Chemie, International Edition published new progress about Alkenylation catalysts (stereoselective, intramol., allylic). 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Product Details of C9H12BClO3.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics