Tag: M.W=150-200

An article Rh(II)-Catalyzed C-H Alkylation of Benzylamines with Unactivated Alkenes: The Influence of Acid on Linear and Branch Selectivity WOS:000661126700036 published article about AROMATIC AMIDES; CATALYZED ALKYLATION; BONDS; DERIVATIVES in [Das, Amrita; Chatani, Naoto] Osaka Univ, Fac Engn, Dept Appl Chem, Suita, Osaka 5650871, Japan in 2021, Cited 47. Category: isothiazole. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

The Rh-catalyzed C-H alkylation of benzylamine derivatives with unactivated 1-alkenes that proceeds via a picolinamide directing group is reported. The crucial role of an acid additive in this transformation is confirmed. Aromatic acids showed high linear selectivity, and aliphatic acids provided branched alkylation products as the major product. The reaction has a broad scope for benzylamines and alkenes. Deuterium labeling experiments suggest that a Rh-carbene intermediate is involved in the case of linear product formation. A different reaction pathway, however, appears to be involved in the case of branched alkylation products, and this pathway also appeared to be a minor pathway in linear-selective reactions.

Category: isothiazole. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Das, A; Chatani, N or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2020 CHEMMEDCHEM published article about CATALYZED SYNTHESIS; SIRTUIN INHIBITORS; IN-VITRO; ELECTROLUMINESCENCE; TRANSMISSION; ENTRY in [Hue, Bui Thi Buu; De, Tran Quang; Van Hieu, Mai; Van Tuan, Nguyen; Anh, Le Duc; Son, Nguyen Hoang; Duc Thanh, Danh La] Can Tho Univ, Coll Nat Sci, Dept Chem, Campus 2,3-2 St, Can Tho City, Vietnam; [Nguyen, Phuong Hong; Jo, Eunji; Thoa, Than Thi; Windisch, Marc P.] Inst Pasteur Korea, Appl Mol Virol Lab, Discovery Biol Div, Seongnam 13488, South Korea; [Nguyen, Phuong Hong; Windisch, Marc P.] Univ Sci & Technol, Div Biomed Sci & Technol, Daejeon 34141, South Korea; [Dupont-Rouzeyrol, Myrielle] Inst Pasteur Nouvelle Caledonie, URE Dengue & Arboviruses, Noumea 98800, New Caledonia; [Grailhe, Regis] Inst Pasteur Korea, Technol Dev Platform, Seongnam 13488, South Korea in 2020, Cited 42. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Safety of 2,5-Dimethoxybenzaldehyde

We have synthesized 50 benzimidazole (BMZ) derivatives with 1,2-phenylenediamines and aromatic aldehydes under mild oxidation conditions by using inexpensive, nontoxic inorganic salt sodium metabisulfite in a one-pot condensation reaction and screened their ability to interfere with Zika virus (ZIKV) infection utilizing a cell-based phenotypic assay. Seven BMZs inhibited an African ZIKV strain with a selectivity index (SI=CC50/EC50) of 9-37. Structure-activity relationship analysis demonstrated that substitution at the C-2, N-1, and C-5 positions of the BMZ ring were important for anti-ZIKV activity. The hybrid structure of BMZ and naphthalene rings was a structural feature responsible for the high anti-ZIKV activity. Importantly, BMZs inhibited ZIKV in human neural stem cells, a physiologically relevant system considering the severe congenital anomalies, like microcephaly, caused by ZIKV infection. Compound 39 displayed the highest antiviral efficacy against the African ZIKV strain in Huh-7 (SI>37) and neural stem cells (SI=12). Compound 35 possessed the highest activity in Vero cells (SI=115). Together, our data indicate that BMZs derivatives have to be considered for the development of ZIKV therapeutic interventions.

Safety of 2,5-Dimethoxybenzaldehyde. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Hue, BTB; Nguyen, PH; De, TQ; Hieu, MV; Jo, E; Tuan, NV; Thoa, TT; Anh, L; Son, NH; Thanh, DLD; Dupont-Rouzeyrol, M; Grailhe, R; Windisch, MP or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Temperini, A; Ballarotto, M; Siciliano, C in [Temperini, Andrea; Ballarotto, Marco] Univ Perugia, Dipartimento Sci Farmaceut, Consorzio CINMPIS, Via Liceo 1, I-06123 Perugia, Italy; [Siciliano, Carlo] Univ Calabria, Dipartimento Farm & Sci Salute & Nutr, Edificio Polifunz, I-87030 Cosenza, Italy published Chemoselective and metal-free reduction of alpha,beta-unsaturated ketones byin situproduced benzeneselenol fromO-(tert-butyl) Se-phenyl selenocarbonate in 2020.0, Cited 59.0. COA of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

The carbon-carbon double bond of arylidene acetones and chalcones can be selectively reduced with benzeneselenol generatedin situby reactingO-(tert-butyl) Se-phenyl selenocarbonate with hydrochloric acid in ethanol. This mild, metal-free and experimentally simple reduction procedure displays considerable functional-group compatibility, products are obtained in good to excellent yields, and the use of toxic Se/CO mixture and NaSeH, or the smelly and air-sensitive benzeneselenol, is avoided.

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Temperini, A; Ballarotto, M; Siciliano, C or concate me.. COA of Formula: C9H10O3

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recently I am researching about CATIONIC-AMPHIPHILIC POLYMERS; PRIMARY ALCOHOLS; MEDICINAL CHEMISTS; DRUG DISCOVERY; BOND FORMATION; PEPTIDE; PHENOLS; REAGENTS; TRANSFORMATION; CONVERSION, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21772150, 22071190]; Wuhan applied fundamental research plan of Wuhan Science and Technology Bureau [2017060201010216]; 111 ProjectMinistry of Education, China – 111 Project; Wuhan University of Technology. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Liu, J; Wang, SM; Qin, HL. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid. COA of Formula: C7H4F2O2

A method for the synthesis of difficult-to-access amides was developed through the coupling of sterically hindered carboxylic acids and electron deficient amines via SO2F2-mediated dehydration. The method feathers with broad substrate scope, mild conditions, excellent functional group compatibility and high yields. (C) 2020 Elsevier Ltd. All rights reserved.

COA of Formula: C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Liu, J; Wang, SM; Qin, HL or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Znidar, D; O’Kearney-McMullan, A; Munday, R; Wiles, C; Poechlauer, P; Schmoelzer, C; Dallinger, D; Kappe, CO in [Znidar, Desiree; Dallinger, Doris; Kappe, C. Oliver] Res Ctr Pharmaceut Engn GmbH RCPE, Ctr Continuous Flow Synth & Proc CCFLOW, Inffeldgasse 13, A-8010 Graz, Austria; [Znidar, Desiree; Dallinger, Doris; Kappe, C. Oliver] Karl Franzens Univ Graz, NAWI Graz, Inst Chem, Heinrichstr 28, A-8010 Graz, Austria; [O’Kearney-McMullan, Anne; Munday, Rachel] AstraZeneca, Silk Rd Business Pk, Macclesfield SK10 2NA, Cheshire, England; [Wiles, Charlotte] Chemtrix BV, Galvaniweg 8A, NL-6101 XH Echt, Netherlands; [Poechlauer, Peter; Schmoelzer, Christoph] Patheon Austria GmbH & Co KG, Sankt Peter Str 25, A-4020 Linz, Austria published Scalable Wolff-Kishner Reductions in Extreme Process Windows Using a Silicon Carbide Flow Reactor in 2019.0, Cited 45.0. COA of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.

A safe and scalable continuous flow strategy for Wolff-Kishner reductions that employs methanol as the solvent has been developed. The use of low-cost hydrazine as the reducing agent in combination with a caustic base provides an atom-efficient, environmentally friendly method for the deoxygenation of aldehydes and ketones to alkanes. Because of the required harsh and corrosive reaction conditions (200 degrees C, 50 bar), reactor materials such as stainless steel, glass, or any type of polymer have compatibility problems, rendering this process problematic on a production scale. The use of corrosion-resistant silicon carbide (SiC) as the reactor material opens up the possibility of performing Wolff-Kishner reductions on scale with a considerably improved safety profile. Methanol as the solvent significantly simplifies the workup procedure compared with the generally employed high-boiling solvents such as diethylene glycol. The continuous flow protocol was applied to a number of substrates and provided the desired products in good to high yields with space-time yields of up to 152 g L(-1)h(-1). In addition, a pharmaceutically valuable active pharmaceutical ingredient precursor was synthesized by employing this high-temperature/pressure Wolff-Kishner protocol.

About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Znidar, D; O’Kearney-McMullan, A; Munday, R; Wiles, C; Poechlauer, P; Schmoelzer, C; Dallinger, D; Kappe, CO or concate me.. COA of Formula: C9H10O3

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Hoffman, RL; Kania, RS; Brothers, MA; Davies, JF; Ferre, RA; Gajiwala, KS; He, MY; Hogan, RJ; Kozminski, K; Li, LLY; Lockner, JW; Lou, JH; Marra, MT; Mitchell, LJ; Murray, BW; Nieman, JA; Noell, S; Planken, SP; Rowe, T; Ryan, K; Smith, GJ; Solowiej, JE; Steppan, CM; Taggart, B in [Hoffman, Robert L.; Kania, Robert S.; Brothers, Mary A.; Davies, Jay F.; Ferre, Rose A.; Gajiwala, Ketan S.; He, Mingying; Kozminski, Kirk; Li, Lilian Y.; Lockner, Jonathan W.; Lou, Jihong; Marra, Michelle T.; Mitchell, Lennert J., Jr.; Murray, Brion W.; Nieman, James A.; Noell, Stephen; Planken, Simon P.; Ryan, Kevin; Smith, George J., III; Solowiej, James E.; Steppan, Claire M.] Pfizer Worldwide Res & Dev, San Diego, CA 92121 USA; [Hogan, Robert J.; Rowe, Thomas; Taggart, Barbara] Southern Res Inst, Birmingham, AL 35205 USA published Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19 in 2020, Cited 45. COA of Formula: C7H4F2O2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1 that caused severe acute respiratory syndrome (SARS) in 2002. Both SARS coronavirus genomes encode two overlapping large polyproteins, which are cleaved at specific sites by a 3C-like cysteine protease (3CL(pro)) in a post-translational processing step that is critical for coronavirus replication. The 3CL(pro) sequences for CoV-1 and CoV-2 viruses are 100% identical in the catalytic domain that carries out protein cleavage. A research effort that focused on the discovery of reversible and irreversible ketone-based inhibitors of SARS CoV-1 3CL(pro) employing ligand-protease structures solved by X-ray crystallography led to the identification of 3 and 4. Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CL(pro) with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

COA of Formula: C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Hoffman, RL; Kania, RS; Brothers, MA; Davies, JF; Ferre, RA; Gajiwala, KS; He, MY; Hogan, RJ; Kozminski, K; Li, LLY; Lockner, JW; Lou, JH; Marra, MT; Mitchell, LJ; Murray, BW; Nieman, JA; Noell, S; Planken, SP; Rowe, T; Ryan, K; Smith, GJ; Solowiej, JE; Steppan, CM; Taggart, B or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recommanded Product: 2,6-Difluorobenzoic acid. Daley, RA; Morrenzin, AS; Neufeldt, SR; Topczewski, JJ in [Daley, Ryan A.; Topczewski, Joseph J.] Univ Minnesota Twin Cities, Dept Chem, Minneapolis, MN 55455 USA; [Morrenzin, Aaron S.; Neufeldt, Sharon R.] Montana State Univ, Dept Chem & Biochem, Bozeman, MT 59717 USA published Gold Catalyzed Decarboxylative Cross-Coupling of Iodoarenes in 2020, Cited 92. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

This report details a decarboxylative cross-coupling of (hetero)aryl carboxylates with iodoarenes in the presence of a gold catalyst (>25 examples, up to 96% yield). This reaction is site specific, which overcomes prior limitations associated with gold catalyzed oxidative coupling reactions. The reactivity of the (hetero)aryl carboxylate correlates qualitatively to the field effect parameter (F-ortho). Reactions with isolated gold complexes and DFT calculations support a mechanism proceeding through oxidative addition at a gold(I) cation with decarboxylation being viable at either a gold(I) or a silver(I) species.

Recommanded Product: 2,6-Difluorobenzoic acid. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Daley, RA; Morrenzin, AS; Neufeldt, SR; Topczewski, JJ or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Liang, XL; Radosevich, M; Loffler, F; Schaeffer, SM; Zhuang, J in [Liang, Xiaolong; Radosevich, Mark; Loffler, Frank; Schaeffer, Sean M.; Zhuang, Jie] Univ Tennessee, Dept Biosyst Engn & Soil Sci, Knoxville, TN 37996 USA; [Loffler, Frank] Univ Tennessee, Dept Microbiol, Dept Civil & Environm Engn, Ctr Environm Biotechnol, Knoxville, TN 37996 USA; [Loffler, Frank] Oak Ridge Natl Lab, Biosci Div, Oak Ridge, TN 37831 USA published Impact of microbial iron oxide reduction on the transport of diffusible tracers and non-diffusible nanoparticles in soils in 2019, Cited 60. Name: 2,6-Difluorobenzoic acid. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.

In subsurface bioremediation, electron donor addition promotes microbial Fe(lII)-oxide mineral reduction that could change soil pore structure, release colloids, and alter soil surface properties. These processes in turn may impact bioremediation rates and the ultimate fate of contaminants. Columns packed with water-stable, Fe-oxide-rich soil aggregates were infused with acetate-containing artificial groundwater and operated for 20 d or 60 d inside an anoxic chamber. Soluble Fe(II) and soil colloids were detected in the effluent within one week after initiation of the acetate addition, demonstrating Fe(III)-bioreduction and colloid formation. Diffusible Br-, less diffusible 2,6-difluorobenzoate (DFBA), and non-diffusible silica-shelled silver nanoparticles (SSSNP) were used as tracers in transport experiments before and after the bioreduction. The transport of Br- was not influenced by the bioreduction. DFBA showed earlier breakthrough and less tailing after the bioreduction, suggesting alterations in flow paths and soil surface chemistry during the 20-d bioreduction treatment. Similarly, the bioreduction increased the transport of SSSNP very significantly, with mass recovery increasing from 1.7% to 25.1%. Unexpectedly, the SSSNP was completely retained in the columns when the acetate injection was extended from 20 to 60 d, while the mass recovery of DFBA decreased from 89.1% to 84.1% and Br showed no change. The large change in the transport of SSSNP was attributed to soil aggregate breakdown and colloid release (causing mechanical straining of SSSNP) and the exposure of iron oxide surfaces previously unavailable within aggregate interiors (facilitating attachment of SSSNP). These results suggest a time dependent fashion of microbial effect on the transport of diffusivity-varying tracers. (C) 2018 Elsevier Ltd. All rights reserved.

About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Liang, XL; Radosevich, M; Loffler, F; Schaeffer, SM; Zhuang, J or concate me.. Name: 2,6-Difluorobenzoic acid

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recently I am researching about PROTEIN-KINASE INHIBITORS; DRUG-RESISTANCE; RECEPTOR 2; GROWTH; BENZOTHIAZOLES; ANGIOGENESIS; DISCOVERY; VEGFR-2; POTENT; MECHANISMS, Saw an article supported by the . Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Abdel-Mohsen, HT; Abd El-Meguid, EA; El Kerdawy, AM; Mahmoud, AEE; Ali, MM. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde. Category: isothiazole

A novel series of 2-arylbenzothiazoles 9, 10, and 12 were designed and synthesized as VEGFR-2/FGFR-1/PDGFR-beta multiangiokinase inhibitors targeting breast cancer. Structural elongation of the known 2-phenylbenzothiazole scaffold (type I protein kinase inhibitor [PKI]), was carried out to afford series of type II PKIs 9, 10, and 12. Compounds 9d, 9f, 9i, and 9k exhibited potent multikinase inhibitory activity with IC50 values of 0.19, 0.18, 0.17, and 0.13 mu M, respectively, against VEGFR-2; IC50 values of 0.28, 0.37, 0.19, and 0.27 mu M, respectively, against FGFR-1; and IC50 values of 0.07, 0.04, 0.08, and 0.14 mu M, respectively, against PDGFR-beta. Moreover, the synthesized benzothiazoles demonstrated promising cytotoxic activity against the MCF-7 cell line. The most potent benzothiazoles 9d and 9i exhibited IC50 values of 7.83 and 6.58 mu M, respectively, on the MCF-7 cell line in comparison to sorafenib (III), which showed IC50 = 4.33 mu M. Additionally, 9d and 9i showed VEGFR-2 inhibitory activity in MCF-7 cells of 81% and 83% when compared with sorafenib (III), which showed 88% inhibition. Molecular docking of the designed compounds in the VEGFR-2 and FGFR-1 active sites showed the accommodation of the 2-phenylbenzothiazole moiety, as reported, in the hinge region of the receptor tyrosine kinase (RTK)-binding site, while the amide moiety is involved in hydrogen bond interactions with the key amino acids in the gate area; this in turn directs the aryl group to the hydrophobic allosteric back pocket of the RTKs in a type II-like binding mode. The synthesized benzothiazoles showed satisfactory ADME properties for further optimization in drug discovery.

Category: isothiazole. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Abdel-Mohsen, HT; Abd El-Meguid, EA; El Kerdawy, AM; Mahmoud, AEE; Ali, MM or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Authors Liu, J; Wang, SM; Qin, HL in PERGAMON-ELSEVIER SCIENCE LTD published article about CATIONIC-AMPHIPHILIC POLYMERS; PRIMARY ALCOHOLS; MEDICINAL CHEMISTS; DRUG DISCOVERY; BOND FORMATION; PEPTIDE; PHENOLS; REAGENTS; TRANSFORMATION; CONVERSION in [Liu, Jing; Qin, Hua-Li] Wuhan Univ Technol, Sch Chem Chem Engn & Life Sci, 205 Luoshi Rd, Wuhan 430070, Peoples R China; [Wang, Shi-Meng] Wuchang Univ Technol, Sch Life Sci, Wuhan 430223, Peoples R China in 2020, Cited 86. Recommanded Product: 2,6-Difluorobenzoic acid. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

A method for the synthesis of difficult-to-access amides was developed through the coupling of sterically hindered carboxylic acids and electron deficient amines via SO2F2-mediated dehydration. The method feathers with broad substrate scope, mild conditions, excellent functional group compatibility and high yields. (C) 2020 Elsevier Ltd. All rights reserved.

Recommanded Product: 2,6-Difluorobenzoic acid. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Liu, J; Wang, SM; Qin, HL or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com