Category: 42413-03-6

Xu, Hui; Zhang, Hong; Tong, Qing-Xiao; Zhong, Jian-Ji published the artcile< Photoredox/cobaloxime co-catalyzed allylation of amines and sulfonyl hydrazides with olefins to access α-allylic amines and allylic sulfones>, Safety of 3-Chloro-4-methylbenzene-1-sulfonyl chloride, the main research area is allylic amine preparation green chem; phenyl tetrahydroisoquinoline methylpropenoate allylation photoredox cobaloxime catalyst; allyl sulfone preparation green chem; sulfonyl hydrazide methyl styrene allylic sulfonylation photoredox cobaloxime catalyst.

A dual-catalytic platform for the allylation of N-phenyltetrahydroisoquinolines I (R = R1 = H, OMe; R2 = H, 3-Me, 2-OMe, 4-Cl) and sulfonyl hydrazides R3SO2NHNH2 (R3 = Ph, cyclopropyl, Pr, etc.) with olefins CH3C(=CH2)R4 (R4 = C(O)OMe, C(O)OCH(CH3)2, C6H5, 4-ClC6H4, etc.) to selectively access α-allylic amines II and allylic sulfones R3SO2CH2C(=CH2)R4 in good yields by combining photoredox catalysis and cobaloxime catalysis was reported. This strategy avoided the use of a stoichiometric amount of terminal oxidant and the use of pre-functionalized allylic precursors, representing a green and ideal atom- & step-economical process. Good substrate scope and gram-scale synthesis demonstrated the utility of this protocol. Mechanistic studies revealed that a radical process is probably involved in this reaction.

Organic & Biomolecular Chemistry published new progress about Allylation. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Safety of 3-Chloro-4-methylbenzene-1-sulfonyl chloride.

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

Ahmed-Belkacem, Rostom; Hausdorff, Marcel; Delpal, Adrien; Sutto-Ortiz, Priscila; Colmant, Agathe M. G.; Touret, Franck; Ogando, Natacha S.; Snijder, Eric J.; Canard, Bruno; Coutard, Bruno; Vasseur, Jean-Jacques; Decroly, Etienne; Debart, Francoise published the artcile< Potent Inhibition of SARS-CoV-2 nsp14 N7-Methyltransferase by Sulfonamide-Based Bisubstrate Analogues>, Category: chlorides-buliding-blocks, the main research area is SARSCoV2 nsp14 methyltransferase inhibitor synthesis COVID19 sulfonamide bisubstrate analog.

Enzymes involved in RNA capping of SARS-CoV-2 are essential for the stability of viral RNA, translation of mRNAs, and virus evasion from innate immunity, making them attractive targets for antiviral agents. In this work, we focused on the design and synthesis of nucleoside-derived inhibitors against the SARS-CoV-2 nsp14 (N7-guanine)-methyltransferase (N7-MTase) that catalyzes the transfer of the Me group from the S-adenosyl-L-methionine (SAM) cofactor to the N7-guanosine cap. Seven compounds out of 39 SAM analogs showed remarkable double-digit nanomolar inhibitory activity against the N7-MTase nsp14. Mol. docking supported the structure-activity relationships of these inhibitors and a bisubstrate-based mechanism of action. The three most potent inhibitors significantly stabilized nsp14 (ΔTm ≈ 11°C), and the best inhibitor demonstrated high selectivity for nsp14 over human RNA N7-MTase.

Journal of Medicinal Chemistry published new progress about Anticoronaviral agents. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Category: chlorides-buliding-blocks.

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

Chen, Xiaohong; Liu, Xiaoguang; Martinez, Jenny S.; Mohr, Justin T. published the artcile< Practical regioselective halogenation of vinylogous esters: synthesis of differentiated mono-haloresorcinols and polyhalogenated resorcinols>, Electric Literature of 42413-03-6, the main research area is regioselective halogenation vinylogous ester; synthesis differentiated haloresorcinol polyhalogenated resorcinol.

A practical and efficient method for the direct, regioselective conversion of vinylogous esters to haloresorcinols is reported. Control of the reaction conditions enables synthesis of either the 4- or 6-haloresorcinol isomers from a common precursor with excellent regiocontrol and high yield. The generality and functional group tolerance of this novel protocol is demonstrated. The utility of this methodol. to access polyhaloresorcinols is also reported. These methods create useful functionalized building blocks for further synthetic applications.

Tetrahedron published new progress about Esters Role: RCT (Reactant), RACT (Reactant or Reagent) (vinylogous). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Electric Literature of 42413-03-6.

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

Lee, Hiu-Fung; Lacbay, Cyrus M.; Boutin, Rebecca; Matralis, Alexios N.; Park, Jaeok; Waller, Daniel D.; Guan, Tian Lai; Sebag, Michael; Tsantrizos, Youla S. published the artcile< Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase>, Name: 3-Chloro-4-methylbenzene-1-sulfonyl chloride, the main research area is multiple myeloma antimyeloma liver toxicity thienopyrimidine hGGPPS inhibitor pharmacokinetics.

Novel analogs of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs) are described that are potent inhibitors of the human geranylgeranyl pyrophosphate synthase (hGGPPS). Members of this class of compounds induce target-selective apoptosis of multiple myeloma (MM) cells and exhibit antimyeloma activity in vivo. A key structural element of these inhibitors is a linker moiety that connects their (((2-phenylthieno[2,3-d]pyrimidin-4-yl)amino)methylene)bisphosphonic acid core to various side chains. The structural diversity of this linker moiety, as well as the side chains attached to it, was investigated and found to significantly impact the toxicity of these compounds in MM cells. The most potent inhibitor CML-07-119(13c)(I) was evaluated in mouse and rat for liver toxicity and systemic exposure, resp., providing further optimism for the potential value of such compounds as human therapeutics.

Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Name: 3-Chloro-4-methylbenzene-1-sulfonyl chloride.

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

Gensini, Martina; Battaglia, Gianluca; Nannicini, Rossano; Guerri, Annalisa; Altamura, Maria; Quartara, Laura published the artcile< Solvent-dependent benzylic radical bromination in aromatic sulfonyl chlorides>, Computed Properties of 42413-03-6, the main research area is bromination toluenesulfonyl chloride derivative solvent effect; bromomethylphenylsulfonyl chloride derivative preparation x ray; crystal structure bromomethylphenylsulfonyl chloride derivative; mol structure bromomethylphenylsulfonyl chloride derivative.

The title reaction of sulfonyl chloride I (R = H) in MeCN gave I (R = Br) with high yield and reproducibility and no byproducts. Three analogs of I (R = H) were similarly brominated.

Letters in Organic Chemistry published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Computed Properties of 42413-03-6.

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

Shinde, Popat S.; Patil, Nitin T. published the artcile< Gold-Catalyzed Dehydrazinative C(sp)-S Coupling Reactions of Arylsulfonyl Hydrazides with Ethynylbenziodoxolones for Accessing Alkynyl Sulfones>, Related Products of 42413-03-6, the main research area is alkynyl sulfone preparation; arylsulfonyl hydrazide preparation ethynylbenziodoxolone dehydrazinative coupling reaction gold catalyst.

A gold(III)-catalyzed dehydrazinative coupling reaction between arylsulfonyl hydrazides RS(O)2NHNH2 (R = C6H5CH2, 5-bromothiophen-2-yl, naphthalen-2-yl, etc.) and ethynylbenziodoxolone reagents I [R1 = Si(CH(CH3)2)3, Si(CH3)2C(CH3)3, Si(C6H5)2C(CH3)3] was realized for the synthesis of alkynyl sulfones RS(O)2CCR1. The scope and versatility of the reaction were demonstrated by the efficient synthesis of 23 derivatives with diverse structural features.

European Journal of Organic Chemistry published new progress about Coupling reaction (C-S). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Related Products of 42413-03-6.

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

Ingle, D. B.; Shingare, M. S. published the artcile< Synthesis of disulfonamides>, Electric Literature of 42413-03-6, the main research area is bactericide disulfonate preparation; sulfonamide bactericide preparation; thiazolesulfonamide benzenesulfonyl; thiophenesulfonamide benzenesulfonyl; coumarin thiophenesulfonamide benzenesulfonyl; acridine thiophenesulfonamide benzenesulfonyl; quinoline thiophenesulfonamide benzenesulfonyl.

RSO2NHSO2R1 (I; R = Ph, Cl-, Br-, Me-, NO2-, CO2H-, AcNH-substituted Ph; R1 = Ph, Cl-, Br-, NO2-, MeO-, AcNH-substituted Ph, 2-thienyl, dimethylthiazolyl, quinolyl, acetamidocoumarinyl) were prepared by amidation of R1SO2Cl with RSO2NH2. I were inactive against S. aureus, S. typhi and V. comma at 200 μg/mL.

Journal of the Indian Chemical Society published new progress about 42413-03-6. 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Electric Literature of 42413-03-6.

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

Spicer, Julie A.; Miller, Christian K.; O’Connor, Patrick D.; Jose, Jiney; Huttunen, Kristiina M.; Jaiswal, Jagdish K.; Denny, William A.; Akhlaghi, Hedieh; Browne, Kylie A.; Trapani, Joseph A. published the artcile< Substituted arylsulphonamides as inhibitors of perforin-mediated lysis>, Recommanded Product: 3-Chloro-4-methylbenzene-1-sulfonyl chloride, the main research area is arylsulfonamide perforin mediated lysis inhibitor structure activity Immunosuppressive; Arylsulphonamide; Bioisostere; Immunosuppressant; Perforin; Perforin inhibitor.

The structure-activity relationships for a series of arylsulfonamide-based inhibitors of the pore-forming protein perforin have been explored. Perforin is a key component of the human immune response, however, inappropriate activity has also been implicated in certain auto-immune and therapy-induced conditions such as allograft rejection and graft vs. host disease. Since perforin is expressed exclusively by cells of the immune system, inhibition of this protein would be a highly selective strategy for the immunosuppressive treatment of these disorders. Compounds from this series were demonstrated to be potent inhibitors of the lytic action of both isolated recombinant perforin and perforin secreted by natural killer cells in vitro. Several potent and soluble examples were assessed for in vivo pharmacokinetic properties and found to be suitable for progression to an in vivo model of transplant rejection.

European Journal of Medicinal Chemistry published new progress about Arenesulfonamides Role: PAC (Pharmacological Activity), PKT (Pharmacokinetics), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Recommanded Product: 3-Chloro-4-methylbenzene-1-sulfonyl chloride.

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

Johnson, Sherida L.; Chen, Li-Hsing; Barile, Elisa; Emdadi, Aras; Sabet, Mojgan; Yuan, Hongbin; Wei, Jun; Guiney, Donald; Pellecchia, Maurizio published the artcile< Structure-activity relationship studies of a novel series of anthrax lethal factor inhibitors>, Reference of 42413-03-6, the main research area is benzothiazole preparation anthrax lethal factor inhibitor SAR.

We report on the identification of a novel small mol. inhibitor of anthrax lethal factor using a high-throughput screening approach. Guided by mol. docking studies, we carried out structure-activity relationship (SAR) studies and evaluated activity and selectivity of most promising compounds in in vitro enzyme inhibition assays and cellular assays. Selected compounds were further analyzed for their in vitro ADME properties, which allowed us to select two compounds for further preliminary in vivo efficacy studies. The data provided represents the basis for further pharmacol. and medicinal chem. optimizations that could result in novel anti-anthrax therapies.

Bioorganic & Medicinal Chemistry published new progress about Anthrax lethal factors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Reference of 42413-03-6.

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

Zhou, Jie; Zhang, Yi; Cui, Yi-Wen; Li, Zhan-Mei; Song, Hong-Rui; Dong, Jin-Hua; Chen, Xiao-Guang; Xu, Bai-Ling published the artcile< Synthesis and cytotoxic evaluation of N-(4-methoxy-1H-benzimidazol-7-yl)arenesulfonamide and N-aryl-(4-methoxy-1H-benzimidazol)-7-sulfonamide analogs of combretastatin A-4>, Computed Properties of 42413-03-6, the main research area is antitumor anticancer agent combretastatin analog preparation.

Benzimidazole derivatives [Combretastatin A-4 2-methoxy-5-[(1Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol analogs] were designed and the synthesis of the target compounds was achieved using 4-methoxy-1H-benzimidazol-7-amine and 4-Methoxy-1H-benzimidazole-7-sulfonic acid as reactants. The title compounds were evaluated in-vitro against cell line HCT-8 (human epithelial intestinal adenocarcinoma, colon carcinoma), cell line BEL-7402 (hepatocellular carcinoma, human hepatoma, liver cancer cell line), cell line BGC 823 (human gastric cancer cell line, stomach adenocarcinoma), cell line A549 (human lung carcinoma cell line) and cell line A-2780 (human ovarian carcinoma cell line) and it was discovered that several compounds displayed cytotoxic activity against the HCT-8 cell line.

Journal of Asian Natural Products Research published new progress about Adenocarcinoma (epithelial adenocarcinoma, intestine). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Computed Properties of 42413-03-6.

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