Category: 35112-05-1

Krupkova, Sona published the artcileSolid-Phase Synthesis of 3-Hydroxy-6-Nitroquinolin-4(1H)-ones with Two Diversity Positions, Product Details of C7H3ClFNO4, the main research area is anthranilic acid chloro resin bound amination esterification cyclization rearrangement; quinolinone hydroxy nitro amino aryl preparation solid phase.

The efficient solid-phase synthesis of 3-hydroxy-2,7-disubstituted-6-nitroquinolin-4(1H)-ones I [R1R2 = (CH2)5, (CH2)2O(CH2)2, R3 = 4-H2N-3,5-Cl2, 4-O2N; etc.] using Rink amide resin was described. The synthesis started from immobilized 4-chloro-5-nitroanthranilic acid, which after nucleophilic replacement of the chlorine atom with various amines R1R2NH and subsequent esterification with bromoacetophenones, afforded substituted phenacyl anthranilates. Their cyclization by heating in sulfuric acid or trifluoroacetic acid gave the corresponding hydroxyquinolinones in excellent purity.

Journal of Combinatorial Chemistry published new progress about Amination. 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Product Details of C7H3ClFNO4.

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

Iniguez, Eva A. published the artcileNovel arylalkylamine compounds exhibits potent selective antiparasitic activity against Leishmania major, Product Details of C7H3ClFNO4, the main research area is arylalkylamine preparation antiparasitic Leishmania leishmaniasis leishmanicide; Amphotericin B; Arylalkylamine compounds; Leishmania major; Mammalian cells.

Leishmania major (L. major) is a protozoan parasite causal agent of Leishmaniasis. It is estimated that 12 million people are currently infected and around 2 million infections occur each year. Current treatments suffer of high toxicity for the patient, low efficacy toward the parasite, high cost, and are losing effectiveness due to parasite resistance. Discovering novel small mol. with high specificity/selectivity and drug-like properties for antileishmanial activity remains a significant challenge. The purpose of this study is to communicate the design and synthesis strategies of novel chem. compounds based of the arylalkylamine scaffold with selective toxicity towards L. major and less toxicity to human cells in vitro. Here, the authors have developed a structure activity relationship (SAR) study of arylalkylamine AA1 in order to study their antiparasitic effect in L. major. Overall, 27 arylalkylamine compounds derived from AA1 were synthesized and purified by silica gel column chromatog. The purity of each analog was confirmed by spectroscopic methods (1H, 13C NMR and LC/MS). Among these analogs, the compound I showed the best toxic activity on L. major (LD50 = 3.34 μM), which represents a 9-fold higher lethality as compared with its parental AA1 (Fer-1) compound (LD50 = 28.75 μM). In addition, I showed no significant toxicity at 80 μM on U20S human osteoblasts, Raw 264.7 Macrophages or i.p. macrophages. In summary, the combined SAR study and biol. evaluation data of AA1-AA27 compounds allow the identification of novel arylalkylamine compound I that exhibits potent cytotoxicity against L. major promastigote with min. toxic effect on human cells.

Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Product Details of C7H3ClFNO4.

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

Krupkova, Sona published the artcile4-Chloro-2-Fluoro-5-Nitrobenzoic Acid as a Possible Building Block for Solid-phase Synthesis of Various Heterocyclic Scaffolds, Category: chlorides-buliding-blocks, the main research area is benzimidazole benzotriazole benzodiazepinedione succinimide solid phase synthesis; benzoic acid chloro fluoro nitro heterocyclic building block.

4-Chloro-2-fluoro-5-nitrobenzoic acid is a com. available multireactive building block that can serve as a starting material in heterocyclic oriented synthesis (HOS) leading to various condensed nitrogenous cycles. This work describes the use of this compound for the preparation of substituted nitrogenous heterocycles having 5-7-membered cycles via polymer-supported o-phenylenediamines. Immobilization of this acid on Rink resin via nucleophilic aromatic substitution of fluorine followed by further chlorine substitution, reduction of a nitro group and appropriate cyclization afforded benzimidazoles, benzotriazoles, quinoxalinones, benzodiazepinediones and succinimides. The method developed is suitable for the synthesis of diverse libraries including the mentioned types of heterocycles, which have significant importance in current drug discovery. The limitations of this method and unsuccessful attempts to prepare an 8-membered benzodiazocine ring are also reported.

ACS Combinatorial Science published new progress about Heterocyclization. 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Category: chlorides-buliding-blocks.

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

Cankarova, Nadezda published the artcileNovel preloaded resins for solid-phase biotinylation of carboxylic acids, Product Details of C7H3ClFNO4, the main research area is carboxylic acid solid phase biotinylation.

Use of solid-phase synthesis for the derivatization of carboxylic acids with biotinylated spacers consisting of ethylenoxy units is described. An aminomethylated resin provided with an acid-labile aldehyde linker is used as the polymer support and three different systems with a reactive amino group are introduced. Acylation of each system was tested with a set of model carboxylic acids and afforded crude products of excellent purity. The preloaded resins are similar to the Biotin-PEG-NovaTagTM resin but offer several advantages including simple elongation of the spacer arm. The protocols described represent a very efficient way of modifying compounds to obtain ligands for affinity chromatog. studies.

Tetrahedron Letters published new progress about Affinity chromatography. 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Product Details of C7H3ClFNO4.

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

Rajapaksa, Naomi S. published the artcileDiscovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity, Application In Synthesis of 35112-05-1, the main research area is preparation benzolactam IRAK4 inhibitor structure.

IRAK4 kinase activity transduces signaling from multiple IL-1Rs and TLRs to regulate cytokines and chemokines implicated in inflammatory diseases. As such, there is high interest in identifying selective IRAK4 inhibitors for the treatment of these disorders. We previously reported the discovery of potent and selective dihydrobenzofuran inhibitors of IRAK4. Subsequent studies, however, showed inconsistent inhibition in disease-relevant pharmacodynamic models. Herein, we describe application of a human whole blood assay to the discovery of a series of benzolactam IRAK4 inhibitors. We identified potent mol. 19 which achieves robust in vivo inhibition of cytokines relevant to human disease.

ACS Medicinal Chemistry Letters published new progress about Enzyme inhibitors (IRAK4). 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Application In Synthesis of 35112-05-1.

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

Wagner, Rolf published the artcileHighlights of the Structure-Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530), Safety of 4-Chloro-2-fluoro-5-nitrobenzoic acid, the main research area is HCV antiviral NS5A inhibition Pibrentasvir analog; benzimidazole linked pyrrolidine Pibrentasvir analog preparation antiviral HCV pharmacokinetics.

Curative interferon and ribavirin sparing treatments for hepatitis C virus (HCV)-infected patients require a combination of mechanistically orthogonal direct acting antivirals. A shared component of these treatments is usually an HCV NS5A inhibitor. First generation FDA approved treatments, including the component NS5A inhibitors, do not exhibit equivalent efficacy against HCV virus genotypes 1-6. In particular, these first generation NS5A inhibitors tend to select for viral drug resistance. Ombitasvir is a first generation HCV NS5A inhibitor included as a key component of Viekira Pak for the treatment of patients with HCV genotype 1 infection. Since the launch of next generation HCV treatments, functional cure for genotype 1-6 HCV infections has been achieved, as well as shortened treatment duration across a wider spectrum of genotypes. In this paper, we show how we have modified the anchor, linker, and end-cap architecture of our NS5A inhibitor design template to discover a next generation NS5A inhibitor pibrentasvir (ABT-530), which exhibits potent inhibition of the replication of wild-type genotype 1-6 HCV replicons, as well as improved activity against replicon variants demonstrating resistance against first generation NS5A inhibitors.

Journal of Medicinal Chemistry published new progress about Anti-hepatitis C virus agents. 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Safety of 4-Chloro-2-fluoro-5-nitrobenzoic acid.

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

Lemrova, Barbora published the artcileSolid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones, Application In Synthesis of 35112-05-1, the main research area is benzodiazepinone solid phase preparation chlorofluoronitrobenzoic acid synthon; benzodiazocinone thiazine thiazepine derivative solid phase preparation.

Solid-phase synthesis of 1,2,3,4-tetrahydro-benzo[e][1,4]diazepin-5-ones with the use of a polystyrene resin is described. The starting material was polymer-supported 1,2-diaminoethane and 4-chloro-2-fluoro-5-nitrobenzoic acid was used as a key synthon. The synthetic approach allows the preparation of derivatives with variable substitution at positions 4 and 8. Addnl., a skeletal diversity was increased when the nitro group was reduced and some benzene fused heterocycles were prepared An expansion of a diazepinone to a benzodiazocinone scaffold was also successful, although some limitations in the diversity of the target derivatives were observed

ACS Combinatorial Science published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Application In Synthesis of 35112-05-1.

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

Xu, Weici published the artcileRestricted Conformation of a Hydrogen Bond Mediated Catalyst Enables the Highly Efficient Enantioselective Construction of an All-Carbon Quaternary Stereocenter, COA of Formula: C7H3ClFNO4, the main research area is all carbon quaternary stereocenter enantioselective Friedel Crafts indole.

A highly active catalyst for the enantioselective Friedel-Crafts alkylation of indoles with β,β-disubstituted nitroalkenes is reported, allowing catalyst loadings down to 0.05 mol % for this challenging transformation, providing useful synthetic building blocks with an all-carbon quaternary stereocenter. The catalyst is based on a bis-cyclometalated iridium(III) complex as a structural template, and through the ligand sphere it forms hydrogen bonds with the two substrates. Starting from a previous design, the catalyst was rendered C2-sym. in order to maximize the atom economy of this catalyst scaffold (two catalytic centers per iridium complex), and, most importantly, rational design was applied to restrict the conformational freedom of a key hydrogen bond acceptor, being responsible for activating the indole nucleophile and bringing it in an ideal position for the presumed ternary transition state.

ACS Catalysis published new progress about Alkenes, nitro Role: RCT (Reactant), RACT (Reactant or Reagent). 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, COA of Formula: C7H3ClFNO4.

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

Kaplanek, Robert published the artcileFast and effective reduction of nitroarenes by sodium dithionite under PTC conditions: application in solid-phase synthesis, Synthetic Route of 35112-05-1, the main research area is nitroarene reduction aryl amine preparation solid phase synthesis; solid phase nitroarene reduction phase transfer catalyst.

Herein, conditions for the fast and effective reduction of aromatic nitro groups bound to hydrophobic polystyrene-based Wang and Rink resins utilizing sodium dithionite in dichloromethane-water under PTC conditions are reported. Tetrabutylammonium hydrogen sulfate (TBAHS) was found to be an effective phase-transfer catalyst for this reaction. This method allows for the reduction of nitro groups to amino groups under mild conditions with complete conversion and is tolerant of other functional groups. This method is a superior alternative to tin(II) chloride-based reduction, which is known for its shortcomings.

Tetrahedron Letters published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Synthetic Route of 35112-05-1.

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