Pecic, Stevan’s team published research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 7079-48-3

Bioorganic & Medicinal Chemistry Letters published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent) (aromatic). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Synthetic Route of 7079-48-3.

Pecic, Stevan published the artcileDesign, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase, Synthetic Route of 7079-48-3, the main research area is sulfonylpiperidinecarboxamide preparation soluble epoxide hydrolase inhibitor antiinflammation antihypertensive.

Inhibition of soluble epoxide hydrolase (sEH) has been proposed as a new pharmaceutical approach for treating hypertension and vascular inflammation. The most potent sEH inhibitors reported in literature to date are urea derivatives However, these compounds have limited pharmacokinetic profiles. We investigated non-urea amide derivatives as sEH inhibitors and identified a potent human sEH inhibitor I having potency comparable to urea-based inhibitors.

Bioorganic & Medicinal Chemistry Letters published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent) (aromatic). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Synthetic Route of 7079-48-3.

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

Kashimura, S.’s team published research in Electrochimica Acta in 1997-04-21 | CAS: 19376-57-9

Electrochimica Acta published new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent). 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Recommanded Product: Methyl 4,4,4-trichlorobutanoate.

Kashimura, S. published the artcileFormation of electrogenerated base by the electroreduction of polyacrylamides, Recommanded Product: Methyl 4,4,4-trichlorobutanoate, the main research area is electrogenerated base electroreduction polyacrylamide; trichloromethylation unsaturated ester electrogenerated base polyacrylamide.

The electroreduction of polyacrylamide derivatives in DMF using tetralkylammonium salts (R4NX) as supporting electrolytes yields the corresponding anionic species possessing interesting reactivities as electrogenerated bases (EGBs). The homopolymer of N-methylacrylamide (MAAm) and its copolymers with N,N-dimethylacrylamide (DMAAm) and styrene (St) were used as polymeric probases and the reactivity of the resulting polymer EGBs was studied. The polymer EGB prepared from the copolymer of MAAm with DMAAm [copoly(MAAm-DMAAm)] containing 65% of MAAm unit gave the best result in the trichloromethylation of α,β-unsaturated esters (89%). Also polymeric probases were easily recovered by reprecipitation and they were repeatedly usable as probases.

Electrochimica Acta published new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent). 19376-57-9 belongs to class chlorides-buliding-blocks, name is Methyl 4,4,4-trichlorobutanoate, and the molecular formula is C5H7Cl3O2, Recommanded Product: Methyl 4,4,4-trichlorobutanoate.

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

Glatt, Hansruedi’s team published research in Archives of Biochemistry and Biophysics in 2008-09-15 | CAS: 36428-96-3

Archives of Biochemistry and Biophysics published new progress about Aldehydes Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Application of Pyrene-2-carboxylic acid.

Glatt, Hansruedi published the artcileDetoxification of promutagenic aldehydes derived from methylpyrenes by human aldehyde dehydrogenases ALDH2 and ALDH3A1, Application of Pyrene-2-carboxylic acid, the main research area is detoxification promutagen pyrene aldehyde human dehydrogenase.

Methylated polycyclic aromatic hydrocarbons can be metabolically activated via benzylic hydroxylation and sulfo conjugation to reactive esters, which can induce mutations and tumors. Yet, further oxidation of the alc. may compete with this toxification. We previously demonstrated that several human alc. dehydrogenases (ADH1C, 2, 3 and 4) oxidize various benzylic alcs. (derived from alkylated pyrenes) to their aldehydes with high catalytic efficiency. However, all these ADHs also catalyzed the reverse reaction, the reduction of the aldehydes to the alcs., with comparable or higher efficiency. Thus, final detoxification requires elimination of the aldehydes by further biotransformation. We have expressed two human aldehyde dehydrogenases (ALDH2 and 3A1) in bacteria. All pyrene aldehydes studied (1-, 2- and 4-formylpyrene, 1-formyl-6-methylpyrene and 1-formyl-8-methylpyrene) were high-affinity substrates for ALDH2 (K m = 0.027-0.9 μM) as well as ALDH3A1 (K m = 0.78-11 μM). Catalytic efficiencies (k cat/K m) were higher for ALDH2 than ALDH3A1 by a moderate to a very large margin depending on the substrate. Most important, they were also substantially higher than the catalytic efficiencies of the various ADHs for the reduction the aldehydes to the alcs. These kinetic properties ensure that ALDHs, and particularly ALDH2, can complete the ADH-mediated detoxification.

Archives of Biochemistry and Biophysics published new progress about Aldehydes Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Application of Pyrene-2-carboxylic acid.

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

Begum, Tahshina’s team published research in European Journal of Organic Chemistry in 2017 | CAS: 61343-99-5

European Journal of Organic Chemistry published new progress about Aromatic ethers Role: SPN (Synthetic Preparation), PREP (Preparation) (biaryl). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application In Synthesis of 61343-99-5.

Begum, Tahshina published the artcilePalladium-on-Carbon-Catalyzed Coupling of Nitroarenes with Phenol: Biaryl Ether Synthesis and Evidence of an Oxidative-Addition-Promoted Mechanism, Application In Synthesis of 61343-99-5, the main research area is nitroarene phenol palladium coupling catalyst; ether biaryl preparation.

Nucleophilic substitution in nitroarenes to form biaryl ethers is of fundamental importance in organic synthesis. Under non-catalytic conditions, this can occur if highly activated nitroarenes are used or if the nucleophile is activated by a strong stoichiometric base. We established a new method involving the use of a ligand-free palladium-on-carbon (Pd/C) catalyst for the cross-coupling of activated nitroarenes with relatively non-nucleophilic phenol derivatives, including naphthol, in the absence of harsh bases. Control experiments, hot filtration, the three-phase test, and inductively coupled plasma at. emission spectroscopy anal. revealed that the catalysis proceeded through an usual oxidative addition step of the nitroarene to Pd/C, which resulted in the release of active palladium particles having extremely high catalytic activity. DFT calculations revealed the origin of the selectivity of the activated nitroarenes.

European Journal of Organic Chemistry published new progress about Aromatic ethers Role: SPN (Synthetic Preparation), PREP (Preparation) (biaryl). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application In Synthesis of 61343-99-5.

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

Takaishi, Kazuto’s team published research in Chemical Science in 2021 | CAS: 36428-96-3

Chemical Science published new progress about Biaryls Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Application In Synthesis of 36428-96-3.

Takaishi, Kazuto published the artcileChiral exciplex dyes showing circularly polarized luminescence: extension of the excimer chirality rule, Application In Synthesis of 36428-96-3, the main research area is chiral exciplex dye circularly polarized luminescence excimer chirality.

A series of axially chiral binaphthyls and quaternaphthyls possessing two kinds of aromatic fluorophores, such as pyrenyl, perylenyl, and 4-(dimethylamino)phenyl groups, arranged alternately were synthesized by a divergent method. In the excited state, the fluorophores selectively formed a unidirectionally twisted exciplex (excited heterodimer) by a cumulative steric effect and exhibited circularly polarized luminescence (CPL). They are the first examples of a monomol. exciplex CPL dye. This versatile method for producing exciplex CPL dyes also improved fluorescence intensity, and the CPL properties were not very sensitive to the solvent or to the temperature owing to the conformationally rigid exciplex. This systematic study allowed us to confirm that the excimer chirality rule can be applied to the exciplex dyes: left- and right-handed exciplexes with a twist angle of less than 90° exhibit (-)- and (+)-CPL, resp.

Chemical Science published new progress about Biaryls Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Application In Synthesis of 36428-96-3.

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

Follows, Bruce’s team published research in Bioorganic & Medicinal Chemistry Letters in 2019-08-15 | CAS: 7079-48-3

Bioorganic & Medicinal Chemistry Letters published new progress about Bid proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

Follows, Bruce published the artcileDiscovery of novel biaryl sulfonamide based Mcl-1 inhibitors, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is Mcl 1 Bid sulfonamide crystal structure; BH3-mimetic; Inhibitors; Mcl-1; Myeloid cell leukemia-1; Small molecule.

Mcl-1 is an anti-apoptotic protein overexpressed in hematol. malignancies and several human solid tumors. Small mol. inhibition of Mcl-1 would offer an effective therapy to Mcl-1 mediated resistance. Subsequently, it has been the target of extensive research in the pharmaceutical industry. The discovery of a novel class of Mcl-1 small mol. inhibitors is described beginning with a simple biaryl sulfonamide hit derived from a high through put screen. A medicinal chem. effort aided by SBDD generated compounds capable of disrupting the Mcl-1/Bid protein-protein interaction in vitro. The crystal structure of the Mcl-1 bound ligand represents a unique binding mode to the BH3 binding pocket where binding affinity is achieved, in part, through a sulfonamide oxygen/Arg263 interaction. The work highlights the some of the key challenges in designing effective protein-protein inhibitors for the Bcl-2 class of proteins.

Bioorganic & Medicinal Chemistry Letters published new progress about Bid proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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

Xu, Jun’s team published research in ChemCatChem in 2018 | CAS: 62593-17-3

ChemCatChem published new progress about Anilines Role: SPN (Synthetic Preparation), PREP (Preparation) (trifluoromethyl). 62593-17-3 belongs to class chlorides-buliding-blocks, name is 2,4-Dichloro-6-(trifluoromethyl)aniline, and the molecular formula is C7H4Cl2F3N, Related Products of chlorides-buliding-blocks.

Xu, Jun published the artcileCoordinating Activation Strategy-Induced Selective C-H Trifluoromethylation of Anilines, Related Products of chlorides-buliding-blocks, the main research area is trifluoromethyl aniline preparation coordinating activation trifluoromethylation picolinamide.

A simple protocol for the synthesis of 2-(trifluoromethyl)aniline derivatives through a coordinating activation strategy was developed. The reaction showed good reactivity and gave the target products in moderate to good yields. Pleasingly, the directing group could be recovered in excellent yield. Furthermore, this strategy allowed efficient access to the synthesis of floctafenine. A single-electron-transfer mechanism was proposed to be responsible for this trifluoromethylation reaction.

ChemCatChem published new progress about Anilines Role: SPN (Synthetic Preparation), PREP (Preparation) (trifluoromethyl). 62593-17-3 belongs to class chlorides-buliding-blocks, name is 2,4-Dichloro-6-(trifluoromethyl)aniline, and the molecular formula is C7H4Cl2F3N, Related Products of chlorides-buliding-blocks.

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

Kas’yan, L. I.’s team published research in Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) in 1997-07-31 | CAS: 7079-48-3

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about Amines Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent) (cage). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

Kas’yan, L. I. published the artcile2-(1-Aminoethyl)bicyclo[2.2.1]heptane. Sulfonamides, ureas, and thioreas on its base, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is aminoethylbicycloheptane conformation electron density nucleophilic reactivity; sulfonamide aminoethylbicycloheptane preparation; urea aminoethylbicycloheptane preparation; thiourea aminoethylbicycloheptane preparation.

The known antiviral drug, 2-(1-aminoethyl)bicyclo[2.2.1]heptane, has been studied by mol. mechanics and quantum-chem. methods. The structure of both exo and endo isomers has been examined by the MMX procedure. Conformational compositions of the isomers and barriers to rotation about the C2-C8 bond have been compared with corresponding parameters of stereoisomeric 2-aminomethylbicyclo[2.2.1]heptanes which also exhibit antiviral activity. The electron d. distribution in the amines has been calculated by the semiempirical AM1 method, and their reactivity has been estimated on the basis of the calculated proton affinities and energies of localized MOs. Nucleophilic properties of the title compound have been studied in reactions with phenylmethane- and arenesulfonyl chlorides and alicyclic and aromatic isocyanates and isothiocyanates. The structure of sulfonamides, ureas, and thioureas thus obtained has been proved by IR and 1H spectroscopy.

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about Amines Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent) (cage). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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

Cho, Sung Jin’s team published research in Journal of Medicinal Chemistry in 2009-04-09 | CAS: 286474-59-7

Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 286474-59-7 belongs to class chlorides-buliding-blocks, name is 6-Chloro-2-fluoro-3-methylbenzaldehyde, and the molecular formula is C8H6ClFO, Formula: C8H6ClFO.

Cho, Sung Jin published the artcileSelective 5-Hydroxytryptamine 2C Receptor Agonists Derived from the Lead Compound Tranylcypromine: Identification of Drugs with Antidepressant-Like Action, Formula: C8H6ClFO, the main research area is serotonin receptor 5HT2c agonist antidepressant tranylcypromine derivative SAR preparation.

We report here the design, synthesis, and pharmacol. properties of a series of compounds related to tranylcypromine (9), which itself was discovered as a lead compound in a high-throughput screening campaign. Starting from 9, which shows modest activity as a 5-HT2C agonist, a series of 1-aminomethyl-2-phenylcyclopropanes was investigated as 5-HT2C agonists through iterative structural modifications. Key pharmacophore feature of this new class of ligands is a 2-aminomethyl-trans-cyclopropyl side chain attached to a substituted benzene ring. Among the tested compounds, several were potent and efficacious 5-HT2C receptor agonists with selectivity over both 5-HT2A and 5-HT2B receptors in functional assays. The most promising compound is 37, with 120- and 14-fold selectivity over 5-HT2A and 5-HT2B, resp. (EC50 = 585, 65, and 4.8 nM at the 2A, 2B, and 2C subtypes, resp.). In animal studies, compound 37 (10-60 mg/kg) decreased immobility time in the mouse forced swim test.

Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 286474-59-7 belongs to class chlorides-buliding-blocks, name is 6-Chloro-2-fluoro-3-methylbenzaldehyde, and the molecular formula is C8H6ClFO, Formula: C8H6ClFO.

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

Wu, Hao’s team published research in Angewandte Chemie, International Edition in 2010 | CAS: 7079-48-3

Angewandte Chemie, International Edition published new progress about 14-3-3 Proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

Wu, Hao published the artcileMicroarray-Assisted High-Throughput Identification of a Cell-Permeable Small-Molecule Binder of 14-3-3 Proteins, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is cell permeable peptide library preparation microarray screening protein binding.

The authors have used a small-mol. microarray (SMM) technique to identify cell-permeable small mol.-peptide hybrids that are capable of binding to all 14-3-3 proteins and thus inhibiting protein-protein interactions (PPI). Phosphoserine-containing peptide libraries were constructed on solid-phase using 243 different carboxylic acids for conjugation with N-terminus of individual peptides in one library, and 50 different amines for conjugation with C-terminus of individual peptides in the second library. For both libraries, biotin and GlyGly linkers were introduced at either N- or C-terminus of each peptide to facilitate subsequent immobilization onto avidin-functionalized glass slides. All the peptide conjugates were characterized by liquid chromatog./mass spectrometry and most were shown to be the correct mol. weight and of sufficient purity for direct microarray applications.

Angewandte Chemie, International Edition published new progress about 14-3-3 Proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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