Category: 3032-32-4

Georgiadis, Taxiarchis M. published the artcileSolid-phase synthesis of an oxalic acid amide library, Related Products of chlorides-buliding-blocks, the main research area is oxalic acid amide library solid phase synthesis; Wang resin bound oxaloyl chloride amidation; arylamine amidation resin bound oxaloyl chloride.

Monoamides of oxalic acid are of interest as bioisosteric replacements for phosphate groups in the design of enzyme inhibitors. The use of oxalic acid as a linker to the Wang resin in the synthesis of individual or libraries of phosphate biosteres is demonstrated. The highly reactive resin-bound acid chloride reacts with arylamines to yield resin-bound N-aryloxamic acids (oxanilic acids). This methodol. is especially useful for the rapid synthesis of 2-(oxalylamino)benzoic acids, because it can be utilized for library synthesis and eliminates the intermediate purification step necessary in solution-phase reactions. The products are cleaved off the resin with trifluoroacetic acid in dichloromethane in good yields.

Journal of Combinatorial Chemistry published new progress about Amidation. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Related Products of chlorides-buliding-blocks.

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

Hradil, Pavel published the artcileSynthesis, NMR spectra and X-ray data of chloro and dichloro derivatives of 3-hydroxy-2-phenylquinolin-4(1H)-ones and their cytostatic activity, Application of 2-Amino-3,6-dichlorobenzoic acid, the main research area is hydroxy phenylquinolinone preparation cytostatic agent.

As known, some derivatives of quinolin-4(1H)-one possess interesting biol. properties. The biol. and cytostatic activity of 2-substituted 3-hydroxyquinolin-4(1H)-ones has not been reported yet. In this paper the synthesis of a series of chloro and dichloro 2-phenyl-3-hydroxyquinolin-4(1H)-ones and their characterization by NMR spectra and X-ray data is described. Their cytostatic properties have been evaluated and the results are reported.

Journal of Heterocyclic Chemistry published new progress about Cyclization. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Application of 2-Amino-3,6-dichlorobenzoic acid.

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

Okuzumi, Tatsuya published the artcileEfficient solid-phase synthesis of quinazoline-2,4-diones with various substituents on aromatic rings, Product Details of C7H5Cl2NO2, the main research area is solid phase synthesis quinazolinedione electron withdrawing substituent; anthranilamide formation solid support cyclization carbonyldiimidazole.

The authors have developed a method for the solid-phase synthesis of quinazoline-2,4-diones with various substituents on the aromatic ring. Although there were numerous reports of the solid-phase synthesis of quinazoline-2,4-diones, they were not applicable to the synthesis of the quinazoline-2,4-diones with electron-withdrawing substituents on the aromatic ring. Considering the poor nucleophilicity of the amino group of anthranilic acids, coupling of anthranilic acids to solid-supported amines was studied without protecting the amino group. Various anthranilamides were prepared using anthranilic acids with electron-withdrawing substituents because a wide range of anthranilic acids are com. available. These anthranilamides were successfully cyclized with carbonyldiimidazole to give quinazoline-2,4-diones with high purity.

Tetrahedron published new progress about Cyclization. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Product Details of C7H5Cl2NO2.

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

Qiu, Li published the artcileReductive Ring Closure Methodology toward Heteroacenes Bearing a Dihydropyrrolo[3,2-b]pyrrole Core: Scope and Limitation, COA of Formula: C7H5Cl2NO2, the main research area is aminobenzoate cyclization chlorination reductive ring closure alkylation; heteroacene dihydropyrrolopyrrole preparation.

A newly developed reductive ring closure methodol. to heteroacenes bearing a dihydropyrrolo[3,2-b]pyrrole core, e.g., I (R = n-octyl), was systematically studied for its scope and limitation. The methodol. involves (i) the cyclization of an o-aminobenzoic acid ester derivative to give an eight-membered cyclic dilactam, and (ii) the conversion of the dilactams into the corresponding diimidoyl chloride, which undergoes (iii) reductive ring closure to install the dihydropyrrolo[3,2-b]pyrrole core. The first step of the methodol. plays the key role due to its substrate limitation, which suffers from the competition of oligomerization and hydrolysis. All the dilactams could successfully convert to the corresponding diimidoyl chlorides, most of which succeeded to give the dihydropyrrolo[3,2-b]pyrrole core. The influence of the substituents and the elongation of conjugated length on the photophys. properties of the obtained heteroacenes were then investigated systematically using UV-vis spectroscopy and cyclic voltammetry. It was found that chlorination and fluorination had quite a different effect on the photophys. properties of the heteroacene, and the ring fusing pattern also had a drastic influence on the band gap of the heteroacene. The successful preparation of a series of heteroacenes bearing a dihydropyrrolo[3,2-b]pyrrole core would provide a wide variety of candidates for further fabrication of organic field-effect transistor devices.

Journal of Organic Chemistry published new progress about Alkylation. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, COA of Formula: C7H5Cl2NO2.

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

Patel, Leena published the artcileDiscovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability, Synthetic Route of 3032-32-4, the main research area is phosphoinositide kinase inhibitor.

Aberrant signaling of phosphoinositide-3-kinase delta (PI3K-delta) has been implicated in numerous pathologies including hematol. malignancies and rheumatoid arthritis. Described in this manuscript is the discovery, optimization and in vivo evaluation of a novel series of pyridine-containing PI3K-delta inhibitors. This work led to the discovery of I, a highly selective inhibitor of PI3K-delta which displays an excellent pharmacokinetic profile and is efficacious in a rodent model of rheumatoid arthritis.

Journal of Medicinal Chemistry published new progress about Antiarthritics. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Synthetic Route of 3032-32-4.

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

Jakobsen, P. published the artcileInhibitors of the tissue factor/factor VIIa-induced coagulation: synthesis and in vitro evaluation of novel specific 2-aryl substituted 4H-3,1-benzoxazin-4-ones, Application of 2-Amino-3,6-dichlorobenzoic acid, the main research area is benzoxazinone preparation structure anticoagulant.

The synthesis of a series of novel 2-aryl substituted 4H-3,1-benzoxazin-4-ones and their evaluation as specific inhibitors of the Tissue Factor (TF)/Factor VIIa (FVIIa)-induced pathway of coagulation is reported. Inhibitory activities (IC50 values) in the range 0.17 to °40 μM on the activation of Factor X (FX) by the TF/FVIIa complex were found for compounds having one or two electroneg. substituents such as F, Cl and NO2 in the 2-aryl substituent. Different substitutions both electron-attracting and donating groups were allowed in the 5, 6, 7 and 8 positions. Several of the compounds showed a selectivity ratio towards FX and thrombin of °50, thus being the first small mols. described as potential drugs for oral antithrombotic treatment without side effects such as bleeding which is observed especially with thrombin inhibitors. The best substituent pattern being the 2-aryl group substituted with: 2-F; 2,6-F2; or 2-FX; 6-Cl; together with electroneg. substitution in the 5, 6, 7, or 8 positions. 2-Heteroaryl substituents like thienyl and furanyl were of low activity while some 2-(2-chloro-3-pyridyl) derivatives had inhibitory activity <10 μM and a good selectivity. Bioorganic & Medicinal Chemistry published new progress about Anticoagulants. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Application of 2-Amino-3,6-dichlorobenzoic acid.

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

Wang, Lijiao published the artcileStable Double and Quadruple [5]Helicene Derivatives: Synthesis, Structural Analysis, and Physical Properties, Application In Synthesis of 3032-32-4, the main research area is pyrene fused indenofluoranthene helicene preparation crystal structure; UV visible spectra lack fluorescence pyrene fused indenofluoranthene helicene; reduction oxidation potential pyrene fused indenofluoranthene helicene.

Pyrene-fused indenofluoranthene helicenes I and II were prepared; the crystal structure of I and the photophys. properties, and oxidation and reduction potentials of I and II were determined Stereoisomerization of the enantiomers and diastereomers of I and II were studied computationally. Chem. oxidation of II with NO+BF4- generated radical cation species at ambient temperature

Organic Letters published new progress about Crystal structure. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Application In Synthesis of 3032-32-4.

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

Evans, Karen A. published the artcileAmino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors, Synthetic Route of 3032-32-4, the main research area is amino acid anthranilamide preparation glycogen phosphorylase inhibitor SAR.

A series of amino acid anthranilamide derivatives identified from a high-throughput screening campaign as novel, potent, and glucose-sensitive inhibitors of human liver glycogen phosphorylase a are described. A solid-phase synthesis using Wang resin was also developed which provided efficient access to a variety of analogs, and resulted in the identification of key structure-activity relationships, and the discovery of the potent exemplar I (IC50 = 80 nM). The SAR scope, synthetic strategy, and in vitro results for this series are presented herein.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Synthetic Route of 3032-32-4.

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

Liang, Rui published the artcileA Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors, HPLC of Formula: 3032-32-4, the main research area is EZH2 inhibitor anticancer blood brain barrier metabolic stability.

Aberrant gene-silencing through dysregulation of polycomb protein activity has emerged as an important oncogenic mechanism in cancer, implicating polycomb proteins as important therapeutic targets. Recently, an inhibitor targeting EZH2, the methyltransferase component of PRC2, received U.S. Food and Drug Administration approval following promising clin. responses in cancer patients. However, the current array of EZH2 inhibitors have poor brain penetrance, limiting their use in patients with central nervous system malignancies, a number of which have been shown to be sensitive to EZH2 inhibition. To address this need, we have identified a chem. strategy, based on computational modeling of pyridone-containing EZH2 inhibitor scaffolds, to minimize P-glycoprotein activity, and here we report the first brain-penetrant EZH2 inhibitor, TDI-6118 (compound 5). Addnl., in the course of our attempts to optimize this compound, we discovered TDI-11904 (compound 21), a novel, highly potent, and peripherally active EZH2 inhibitor based on a 7 member ring structure.

ACS Medicinal Chemistry Letters published new progress about Antiproliferative agents. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, HPLC of Formula: 3032-32-4.

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

Okuzumi, Tatsuya published the artcileEfficient solid-phase synthesis of diverse 1,2,3-benzotriazin-4-ones using tert-butyl nitrite, HPLC of Formula: 3032-32-4, the main research area is solid phase combinatorial synthesis benzotriazinone derivative aminobenzamide diazotization cyclization.

The solid-phase synthesis of 1,2,3-benzotriazin-4-ones, e.g. I, via the intramol. cyclization of 2-aminobenzamides through diazotization using tert-Bu nitrite is reported. Addnl., a small library of 1,2,3-benzotriazin-4-ones was combinatorially prepared utilizing this methodol. In view of the fact that this library contains three points of diversity, the preparation of a large number of compounds is possible.

Tetrahedron Letters published new progress about Combinatorial chemistry. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, HPLC of Formula: 3032-32-4.

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