Category: 350-30-1

Wu, Yun; Wang, Beilei; Wang, Junjie; Qi, Shuang; Zou, Fengming; Qi, Ziping; Liu, Feiyang; Liu, Qingwang; Chen, Cheng; Hu, Chen; Hu, Zhenquan; Wang, Aoli; Wang, Li; Wang, Wenchao; Ren, Tao; Cai, Yujiao; Bai, Mingfeng; Liu, Qingsong; Liu, Jing published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors》.Recommanded Product: 350-30-1 The author mentioned the following in the article:

Starting from our previously developed c-KIT kinase inhibitor CHMFL-KIT-8140, through a type II kinase inhibitor binding element hybrid design approach, we discovered a novel c-KIT kinase inhibitor compound 18 (CHMFL-KIT-64), which is potent against c-KIT wt and a broad spectrum of drug-resistant mutants with improved bioavailability. 18 exhibits single-digit nM potency against c-KIT kinase and c-KIT T670I mutants in the biochem. assay and displays great potencies against most of the gain-of-function mutations in the juxtamembrane domain, drug-resistant mutations in the ATP binding pocket (except V654A), and activation loops (except D816V). In addition, 18 exhibits a good in vivo pharmacokinetic (PK) profile in different species including mice, rats, and dogs. It also displays good in vivo antitumor efficacy in the c-KIT T670I, D820G, and Y823D mutant-mediated mice models as well as in the c-KIT wt patient primary cells which are known to be imatinib-resistant. The potent activity against a broad spectrum of clin. important c-KIT mutants combining the good in vivo PK/pharmacodynamic properties of 18 indicates that it might be a new potential therapeutic candidate for gastrointestinal stromal tumors. The results came from multiple reactions, including the reaction of 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Recommanded Product: 350-30-1)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. Recommanded Product: 350-30-1 The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.

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

Application In Synthesis of 3-Chloro-4-fluoronitrobenzeneOn March 31, 2019, Isaka, Masahiko; Yangchum, Arunrat; Supothina, Sumalee; Veeranondha, Sukitaya; Komwijit, Somjit; Phongpaichit, Souwalak published an article in Journal of Antibiotics. The article was 《Semisynthesis and antibacterial activities of nidulin derivatives》. The article mentions the following:

Derivatives of the fungal depsidone, nidulin, have been synthesized in order to evaluate the potential of the chem. skeleton as antibacterial agents. Alkylation, acylation, and arylation reactions of nornidulin underwent in a regioselective manner to predominantly produce 8-O-substituted derivatives Many of the semisynthetic derivatives showed more potent antibacterial activities than nidulin, In particular, 8-O-aryl ether derivatives displayed significant activities against Gram-pos. bacteria, including Methicillin-resistant Staphylococcus aureus. In the experiment, the researchers used 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Application In Synthesis of 3-Chloro-4-fluoronitrobenzene)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Application In Synthesis of 3-Chloro-4-fluoronitrobenzene

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

Li, Shan; Si, Hongfei; Song, Xiaojuan; Lei, Chong; He, Xiaoqiang; Wang, Jie; Liu, Yiling; Zhou, Yang; Song, Jian-Guo; Peng, Lijie; Tang, Xia; Chan, Shingpan; Ren, Xiaomei; Tu, Zhengchao; Li, Zhengqiu; Wang, Zhen; Zhang, Zhang; Ding, Ke published their research in Journal of Medicinal Chemistry on August 11 ,2022. The article was titled 《Discovery of Hexahydrofuro[3,2-b]furans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant》.Application of 350-30-1 The article contains the following contents:

Janus kinase 3 (JAK3) is a potential target for the treatment of hematol. malignancies. Herein, we report the discovery of a series of new orally bioavailable irreversible JAK3 kinase inhibitors. The representative compound 12n (I) potently inhibited JAK3 kinase activity with an IC50 value of 1.2 nM and was more than 900-fold selective over JAK1, JAK2, and Tyk2. Cell-based assays revealed that 12n significantly suppressed phosphorylation of JAK3 and the downstream effectors STAT3/5 and also robustly restrained proliferation of BaF3 cells transfected with JAK3M511I activating mutation and human leukemia U937 cells harboring JAK3M511I with IC50 values of 22.9 and 20.2 nM, resp. More importantly, 12n showed reasonable pharmacokinetic (PK) properties, and oral administration of 12n at a dose of 50 mg/kg twice daily led to tumor regression in a U937 cell inoculated xenograft mouse model. Thus, 12n represents a promising lead compound for further optimization to discover new therapeutic agents for hematol. malignancies. In addition to this study using 3-Chloro-4-fluoronitrobenzene, there are many other studies that have used 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Application of 350-30-1) was used in this study.

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Application of 350-30-1

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

Dai, Yihu; Jiang, Chunyang; Xu, Min; Bian, Bo; Lu, Di; Yang, Yanhui published an article in Applied Catalysis, A: General. The title of the article was 《Cobalt in N-doped carbon matrix catalyst for chemoselective hydrogenation of nitroarenes》.Category: chlorides-buliding-blocks The author mentioned the following in the article:

Anilines as important intermediates for both organic synthesis and industrial manufactory are densely substituted with a variety of functional moieties, and the transformation of nitroarenes into corresponding anilines requires catalytically selective hydrogenation catalyst. Herein, we describe a simple pyrolysis strategy to prepare cobalt catalysts in nitrogen-doped carbon matrix applied in the selective hydrogenation of nitroarenes with mol. hydrogen. The Co/NC catalysts are obtained through thermal treatment of mixed precursors of cobalt phthalocyanine and melamine. The surface-modified Co particles with Co3O4 and CoNx sites are surrounded by N-doped carbon layers according to a series of structural characterization results. These Co/NC catalysts are capable of efficiently selective hydrogenation of nitrobenzene and various substituted nitroarenes into corresponding anilines under relatively mild reaction conditions. The optimal catalytic hydrogenation performance is contributed to the fast rate of H2 dissociated activation on the CoNx active sites and the facile adsorption of the reactant substances, which is verified by the isotopic H2-D2 exchange experiments, reactant adsorption and the ORR reaction tests. Furthermore, the heterogeneous Co/NC catalyst is highly stable without the Co leaching and deactivation issues during the recycling reaction runs. The experimental part of the paper was very detailed, including the reaction process of 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Category: chlorides-buliding-blocks)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.Category: chlorides-buliding-blocks

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

The author of 《Palladium-catalyzed reductive desulfonative aminocarbonylation of benzylsulfonyl chlorides with nitroarenes towards arylacetamides》 were Liu, Yongzhu; Bao, Zhi-Peng; Qi, Xinxin; Wu, Xiao-Feng. And the article was published in Organic Chemistry Frontiers in 2022. Product Details of 350-30-1 The author mentioned the following in the article:

A new palladium-catalyzed reductive desulfonative aminocarbonylation reaction with benzylsulfonyl chlorides RCH2S(O)2Cl (R = Ph, 3,4-dimethylphenyl, 2,4-dichlorophenyl, etc.) as C(sp3) electrophiles has been developed. Using nitroarenes R1NO2 (R1 = Ph, quinolin-8-yl, 2H-1,3-benzodioxol-5-yl, etc.) as readily accessible and stable nitrogen surrogates, a wide range of arylacetamides RCH2C(O)NHR1 were easily prepared in high yields with very good functional group compatibility. Mo(CO)6 plays a dual role as both a CO source and reductant. Moreover, a late-stage modification of natural products was also achieved via this aminocarbonylation strategy. The experimental part of the paper was very detailed, including the reaction process of 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Product Details of 350-30-1)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Product Details of 350-30-1

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

Electric Literature of C6H3ClFNO2On May 12, 2022 ,《Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations》 appeared in Journal of Medicinal Chemistry. The author of the article were Chen, Hao; Lai, Mengzhen; Zhang, Tao; Chen, Yuqing; Tong, Linjiang; Zhu, Sujie; Zhou, Yang; Ren, Xiaomei; Ding, Jian; Xie, Hua; Lu, Xiaoyun; Ding, Ke. The article conveys some information:

Tertiary C797S mutation of epidermal growth factor receptor (EGFR)-mediated resistance in non-small-cell-lung-cancer (NSCLC) patients is still an unmet clin. need. Several classes of ATP-competitive or allosteric EGFRT790M/C797S inhibitors and degraders have been developed, but none of them have received approval from the regulatory agencies. Herein, we report the structure-based design of conformational constrained 4-(1-ethylsufonyl-3-indolyl)-2-phenylaminopyrimidines as new EGFRT790M/C797S inhibitors by using a macrocyclization strategy. Representative compound 18j potently inhibited EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S mutants with IC50 values of 15.8 and 23.6 nM and suppressed Ba/F3-EGFRL858R/T790M/C797S and Ba/F3-EGFR19del/T790M/C797S cells with IC50 values of 0.036 and 0.052 μM, resp., which is 10-20-fold more potent than brigatinib. 18j also potently inhibited the EGFR19del/T790M/C797S-mutated PC-9-OR NSCLC cell proliferation with an IC50 value of 0.644 μM but was less potent for parental Ba/F3 and A431 cells. This study provides a new lead compound for drug discovery to combat EGFRC797S-mediated resistance in NSCLC patients. In the part of experimental materials, we found many familiar compounds, such as 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Electric Literature of C6H3ClFNO2)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties.Electric Literature of C6H3ClFNO2 Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.

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

《Palladium Catalyzed Aminocarbonylation of Benzylic Ammonium Triflates with Nitroarenes: Synthesis of Phenylacetamides》 was written by Yang, Li-Miao; Li, Shan-Shan; Zhang, You-Ya; Lu, Jin-Liang; Deng, Jing-Tong; Ma, Ai-Jun; Zhang, Xiang-Zhi; Zhang, Shu-Yu; Peng, Jin-Bao. Recommanded Product: 350-30-1 And the article was included in Advanced Synthesis & Catalysis on April 17 ,2021. The article conveys some information:

A palladium catalyzed reductive aminocarbonylation of benzylic ammonium triflates with nitroarenes for the synthesis of phenylacetamides was developed. Using Pd(acac)2/DPPF catalyst system, a range of different substituted phenylacetamides were prepared in moderate to good yields from benzylic ammonium triflates and nitroarenes through Csp3-N bond cleavage. A variety of alkyl, aryl, and halide substituents on both substrates was used, and many useful functional groups were tolerated. In the experiment, the researchers used many compounds, for example, 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Recommanded Product: 350-30-1)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 350-30-1

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

Blake, Steven; Thanissery, Rajani; Rivera, Alissa J.; Hixon, Mark S.; Lin, Mingliang; Theriot, Casey M.; Janda, Kim D. published an article in Journal of Medicinal Chemistry. The title of the article was 《Salicylanilide Analog Minimizes Relapse of Clostridioides difficile Infection in Mice》.Product Details of 350-30-1 The author mentioned the following in the article:

Clostridioides difficile infection (CDI) causes serious and sometimes fatal symptoms like diarrhea and pseudomembranous colitis. Although antibiotics for CDI exist, they are either expensive or cause recurrence of the infection due to their altering the colonic microbiota, which is necessary to suppress the infection. Here, we leverage a class of known membrane-targeting compounds that we previously showed to have broad inhibitory activity across multiple Clostridioides difficile strains while preserving the microbiome to develop an efficacious agent. A new series of salicylanilides was synthesized, and the most potent analog was selected through an in vitro inhibitory assay to evaluate its pharmacokinetic parameters and potency in a CDI mouse model. The results revealed reduced recurrence of CDI and diminished disturbance of the microbiota in mice compared to standard-of-care vancomycin, thus paving the way for novel therapy that can potentially target the cell membrane of C. difficile to minimize relapse in the recovering patient. After reading the article, we found that the author used 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Product Details of 350-30-1)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.Product Details of 350-30-1

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

Elwaie, Tamer A.; Abbas, Safinaz E.; Aly, Enayat I.; George, Riham F.; Ali, Hamdy; Kraiouchkine, Nikolai; Abdelwahed, Khaldoun S.; Fandy, Tamer E.; El Sayed, Khalid A.; Abd Elmageed, Zakaria Y.; Ali, Hamed I. published their research in Journal of Medicinal Chemistry on December 24 ,2020. The article was titled 《HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability》.Product Details of 350-30-1 The article contains the following contents:

HER2 kinase as a well-established target for breast cancer (BC) therapy is associated with aggressive clin. outcomes; thus, herein we present structural optimization for HER2-selective targeting. HER2 profiling of the developed derivatives demonstrated potent and selective inhibitions (IC50: 5.4-12 nM) compared to lapatinib (IC50: 95.5 nM). Favorably, 17d exhibited min. off-target kinase activation. NCI-5-dose screening revealed broad-spectrum activities (GI50: 1.43-2.09μM) and 17d had a remarkable selectivity toward BC. Our compounds revealed significant selective and potent antiproliferative activities (~20-fold) against HER2+ (AU565, BT474) compared to HER2(-) cells. At 0.1 IC50, 15i, 17d, and 25b inhibited pERK1/2 and pAkt by immunoblotting. Furthermore, 17d demonstrated potent in vivo tumor regression against the BT474 xenograft model. Notably, a metastasis case was observed in the vehicle but not in the test mice groups. CD-1 mice metabolic stability assay revealed high stability and low intrinsic clearance of 17d (T1/2 > 145 min and CLint(mic) < 9.6 mL/min/kg). The experimental process involved the reaction of 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Product Details of 350-30-1)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties.Product Details of 350-30-1 Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.

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

Related Products of 350-30-1On March 31, 2021, Chen, Jinyi; Wang, Hongxing published an article in Journal of Chemical Thermodynamics. The article was 《Density, viscosity, and saturated vapour pressure of 3-chloro-4-fluoronitrobenzene and 3-chloro-2-fluoronitrobenzene》. The article mentions the following:

D. and viscosity data of pure 3-chloro-4-fluoronitrobenzene and 3-chloro-2-fluoronitrobenzene were obtained in temperature range from 318.15 K to 348.15 K at the local atm. pressure of 99.7 kPa. The value of corresponding saturated vapor pressure of two isomers were determined in the temperature range of 409 K to 517 K. The relationship between temperature and d. can be well correlated by the linear equation. The viscosity data was well described by the Litovitz, Ghatee, VFT, and Andrade equations, and the calculated value by the VFT equation is consistent with the measured data. Both the Antoine and Riedel equations can accurately describe the relationship between saturated vapor pressure and temperature of 3-chloro-4-fluoronitrobenzene and 3-chloro-2-fluoronitrobenzene, which can meet the requirements for chem. design. In addition, the thermal expansion coefficient was determined based on the d. data, and the molar vaporisation enthalpy of two isomers was evaluated using the Clausius-Clapeyron equation. In the experimental materials used by the author, we found 3-Chloro-4-fluoronitrobenzene(cas: 350-30-1Related Products of 350-30-1)

3-Chloro-4-fluoronitrobenzene(cas: 350-30-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.Related Products of 350-30-1

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