Category: 329-59-9

In 2012,Alorati, Anthony D.; Gibb, Andrew D.; Mullens, Peter R.; Stewart, Gavin W. published 《An Efficient Process for the Large-Scale Synthesis of a 2,3,6-Trisubstituted Indole》.Organic Process Research & Development published the findings.Synthetic Route of C8H6FNO4 The information in the text is summarized as follows:

The efficient synthesis of a key trisubstituted indole intermediate 1 is described. The synthetic route required the use of an aryl Grignard reagent which was not com. available, and the large-scale formation of this fragment and the thermal evaluation for this step is presented. The key step in the sequence was a Truce-Smiles rearrangement to provide an advanced ketone intermediate which, upon reduction, cyclized to the desired indole 1. Design of experiment (DoE) optimization of this reduction is also presented. In total >50 kg of target indole 1 were synthesized in 55% overall yield over five steps using this new route. In the experimental materials used by the author, we found Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Synthetic Route of C8H6FNO4)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Synthetic Route of C8H6FNO4Methyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2016,Read, Cai; Fitzpatrick, Christopher M.; Yang, Peiran; Kuc, Rhoda E.; Maguire, Janet J.; Glen, Robert C.; Foster, Richard E.; Davenport, Anthony P. published 《Cardiac action of the first G protein biased small molecule apelin agonist》.Biochemical Pharmacology (Amsterdam, Netherlands) published the findings.Computed Properties of C8H6FNO4 The information in the text is summarized as follows:

Apelin peptide analogs displaying bias towards G protein signalling pathways have beneficial cardiovascular actions compared with the native peptide in humans in vivo. Our aim was to determine whether small mol. agonists could retain G protein bias. We have identified a biased small mol., CMF-019 (I), and characterised it in vitro and in vivo. In competition radioligand binding experiments in heart homogenates, CMF-019 bound to the human, rat and mouse apelin receptor with high affinity (pKi = 8.58 ± 0.04, 8.49 ± 0.04 and 8.71 ± 0.06 resp.). In cell-based functional assays, whereas, CMF-019 showed similar potency for the Gαi pathway to the endogenous agonist [Pyr1]apelin-13 (pD2 = 10.00 ± 0.13 vs 9.34 ± 0.15), in β-arrestin and internalisation assays it was less potent (pD2 = 6.65 ± 0.15 vs 8.65 ± 0.10 and pD2 = 6.16 ± 0.21 vs 9.28 ± 0.10 resp.). Anal. of these data demonstrated a bias of ∼400 for the Gαi over the β-arrestin pathway and ∼6000 over receptor internalisation. CMF-019 was tested for in vivo activity using i.v. injections into anesthetized male Sprague-Dawley rats fitted with a pressure-volume catheter in the left ventricle. CMF-019 caused a significant increase in cardiac contractility of 606 ± 112 mmHg/s (p < 0.001) at 500 nmol. CMF-019 is the first biased small mol. identified at the apelin receptor and increases cardiac contractility in vivo. We have demonstrated that Gαi over β-arrestin/internalisation bias can be retained in a non-peptide analog and predict that such bias will have the therapeutic benefit following chronic use. CMF-019 is suitable as a tool compound and provides the basis for design of biased agonists with improved pharmacokinetics for treatment of cardiovascular conditions such as pulmonary arterial hypertension. The experimental process involved the reaction of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Computed Properties of C8H6FNO4)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Computed Properties of C8H6FNO4Methyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG)》 was written by Tsagris, Denise J.; Birchall, Kristian; Bouloc, Nathalie; Large, Jonathan M.; Merritt, Andy; Smiljanic-Hurley, Ela; Wheldon, Mary; Ansell, Keith H.; Kettleborough, Catherine; Whalley, David; Stewart, Lindsay B.; Bowyer, Paul W.; Baker, David A.; Osborne, Simon A.. Synthetic Route of C8H6FNO4This research focused ontrisubstituted thiazole preparation Plasmodium protein kinase G inhibitor; Malaria; PfPKG; Plasmodium falciparum; Thiazole. The article conveys some information:

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria. After reading the article, we found that the author used Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Synthetic Route of C8H6FNO4)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Synthetic Route of C8H6FNO4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2009,Gowda, N. R. Thimme; Kavitha, C. V.; Chiruvella, Kishore K.; Joy, Omana; Rangappa, Kanchugarakoppal S.; Raghavan, Sathees C. published 《Synthesis and biological evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives and their precursors as antileukemic agents》.Bioorganic & Medicinal Chemistry Letters published the findings.Related Products of 329-59-9 The information in the text is summarized as follows:

The synthesis and preliminary evaluation of novel 1-(4-methoxyphenethyl)-1H-benzimidazole-5-carboxylic acid derivatives and their precursors as potential chemotherapeutic agents are reported. In each case, the structures of the compounds were determined by FTIR, 1H NMR, and mass spectroscopy. Among the synthesized mols., Me 1-(4-methoxyphenethyl)-2-(4-fluoro-3-nitrophenyl)-1H-benzimidazole-5-carboxylate (I) induced maximum cell death in leukemic cells with an IC50 value of 3 μM. FACS anal. shows that the compound I induces S/G2 cell cycle arrest, which was further supported by the observed down regulation of CDK2, Cyclin B1, and PCNA. The observed downregulation of proapoptotic proteins, upregulation of antiapoptotic proteins, cleavage of PARP, and elevated levels of DNA strand breaks indicated the activation of apoptosis by I. These results suggest that I could be a potent anti-leukemic agent. In the experimental materials used by the author, we found Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Related Products of 329-59-9)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Related Products of 329-59-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2010,El-Essawi, Aschraf; Hajek, Tomas; Skorpil, Jirji; Böning, Andreas; Sabol, Frantisek; Hausmann, Harald; Ostrovsky, Yuri; Harringer, Wolfgang published 《A prospective randomised multicentre clinical comparison of a minimised perfusion circuit versus conventional cardiopulmonary bypass.》.European journal of cardio-thoracic surgery published the findings.HPLC of Formula: 329-59-9 The information in the text is summarized as follows:

OBJECTIVE: Minimised perfusion circuits (MPCs) are expected to reduce the side effects of conventional cardiopulmonary bypass (CCPB); however, conclusive data from sufficiently powered clinical trials are lacking. The purpose of this study was to evaluate the safety and efficacy of the ROCsafeRX minimised perfusion circuit. METHODS: A randomised, controlled, multicentre clinical trial comparing both perfusion circuits in patients subjected to elective coronary artery bypass and/or aortic valve replacement is described. The primary end points of safety, defined as procedure success without device-related complications, and secondary end point of efficacy, including reduction of transfusion requirement and incidence of atrial fibrillation, are analysed. RESULTS: To date, 291 patients have been enrolled and randomised (146 MPC vs 145 CCPB). With the exception of a significantly higher male population in the MPC group (83.6% vs 71.0%, p=0.01), both groups were well matched for demographic data and type of surgery. There were no device-related complications but a hard-shell reservoir had to be integrated in one MPC because of a tear in the right atrium that was managed uneventfully. Total transfusion requirement (329+/-599 ml vs 783+/-1638 ml, p < or = 0.001) and erythrocyte transfusion (181+/-341 ml vs 434+/-798 ml, p < or = 0.001) were significantly reduced in the MPC group. The incidence of atrial fibrillation was significantly lower in the MPC group (7.1% vs 19.5%, p < or = 0.01), while freedom of major adverse events showed no significant difference. CONCLUSIONS: Lack of device-related complications combined with a significant reduction in postoperative atrial fibrillation and transfusion requirements have shown the ROCsafeRX MPC to be both safe and efficient for large-scale use in cardiac patients. Additional data are expected to confirm these initial findings. The experimental part of the paper was very detailed, including the reaction process of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9HPLC of Formula: 329-59-9)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.HPLC of Formula: 329-59-9Methyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2013,Lentz, Christian S.; Halls, Victoria; Hannam, Jeffrey S.; Niebel, Bjoern; Struebing, Uta; Mayer, Guenter; Hoerauf, Achim; Famulok, Michael; Pfarr, Kenneth M. published 《A Selective Inhibitor of Heme Biosynthesis in Endosymbiotic Bacteria Elicits Antifilarial Activity In Vitro》.Chemistry & Biology (Oxford, United Kingdom) published the findings.COA of Formula: C8H6FNO4 The information in the text is summarized as follows:

Lymphatic filariasis and onchocerciasis are severe diseases caused by filarial worms and affect more than 150 million people worldwide. Endosymbiotic α-proteobacteria Wolbachia are essential for these parasites throughout their life cycle. Using a high-throughput chem. screen, we identified a benzimidazole compound, wALADin1, that selectively targets the δ-aminolevulinic acid dehydratase (ALAD) of Wolbachia (wALAD) and exhibits macrofilaricidal effects on Wolbachia-containing filarial worms in vitro. wALADin1 is a mixed competitive/noncompetitive inhibitor that interferes with the Mg2+-induced activation of wALAD. This mechanism inherently excludes activity against the Zn2+-dependent human ortholog and might be translatable to Mg2+-responsive orthologs of other bacterial or protozoan pathogens. The specificity profile of wALADin1 derivatives reveals chem. features responsible for inhibitory potency and species selectivity. Our findings validate wALADins as a basis for developing potent leads that meet current requirements for antifilarial drugs. The results came from multiple reactions, including the reaction of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9COA of Formula: C8H6FNO4)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.COA of Formula: C8H6FNO4Methyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2018,Medicinal Chemistry (Sharjah, United Arab Emirates) included an article by Trifonov, Lena; Afri, Michal; Palczewski, Krzysztof; Korshin, Edward E.; Gruzman, Arie. COA of Formula: C8H6FNO4. The article was titled 《An Expedient Synthesis of CMF-019: (S)-5-Methyl-3-{1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido}hexanoic Acid, a Potent Apelin Receptor (APJ) Agonist》. The information in the text is summarized as follows:

Here, a detailed preparation of (S)-5-methyl-3-{1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido}hexanoic acid (CMF-019) (I) through a modified and improved synthetic pathway was described. The results came from multiple reactions, including the reaction of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9COA of Formula: C8H6FNO4)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.COA of Formula: C8H6FNO4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2013,Yellol, Gorakh S.; Donaire, Antonio; Yellol, Jyoti G.; Vasylyeva, Vera; Janiak, Christoph; Ruiz, Jose published 《On the antitumor properties of novel cyclometalated benzimidazole Ru(ii), Ir(iii) and Rh(iii) complexes》.Chemical Communications (Cambridge, United Kingdom) published the findings.Related Products of 329-59-9 The information in the text is summarized as follows:

Smart design and efficient synthesis of benzimidazole Ru, Ir and Rh cyclometalated complexes are reported with promising cytotoxic activity against HT29, T47D, A2780 and A2780cisR cancer cell lines. Their apoptosis, accumulation, cell cycle arrest, protein binding and DNA binding effects are also discussed. In the experiment, the researchers used many compounds, for example, Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Related Products of 329-59-9)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Related Products of 329-59-9Methyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2004,Andrews, Stephen P.; Joensson, Daniel; Warrington, Brian H.; Ladlow, Mark published 《Automated parallel, multi-step polymer-assisted solution phase (PASP) synthesis of substituted benzimidazole derivatives》.Combinatorial Chemistry and High Throughput Screening published the findings.Reference of Methyl 4-fluoro-3-nitrobenzoate The information in the text is summarized as follows:

The automated polymer-assisted solution phase (PASP) synthesis of a 72 member library of 1-R1-2-R2S-5-R3C(O)benzimidazoles (e.g. 2-(benzylthio)-1-sec-butyl-5-(cyclopentylcarbamoyl)benzimidazole) and 1-R1-3-R2-5-R3C(O)benzimidazol-2(3H)-ones (e.g. 3-benzyl-1-sec-butyl-5-(cyclopentylcarbamoyl)-1H-benzimidazol-2(3H)-one) using com. available robotic workstations is described. By incorporating both automated aqueous work-ups, in-line scavenging and catch and release protocols the desired compounds were obtained directly in good yields and excellent purities without the need for conventional chromatog. purification The synthesis described demonstrates how both manual and automated equipment may be used together to provide a versatile approach that facilitates parallel compound synthesis. In addition to this study using Methyl 4-fluoro-3-nitrobenzoate, there are many other studies that have used Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Reference of Methyl 4-fluoro-3-nitrobenzoate) was used in this study.

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Reference of Methyl 4-fluoro-3-nitrobenzoateMethyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2016,Selvaraju, Manikandan; Ye, Tzuen-Yang; Li, Chia-Hsin; Ho, Pei-Heng; Sun, Chung-Ming published 《Copper catalyzed aerobic oxidative cyclization and ketonization: one pot synthesis of benzoimidazo[1,2-a]imidazolones》.Chemical Communications (Cambridge, United Kingdom) published the findings.Recommanded Product: Methyl 4-fluoro-3-nitrobenzoate The information in the text is summarized as follows:

A highly efficient synthesis of benzoimidazo[1,2-a]imidazolone I [R1 = 6-CH3, 6-C(O)OCH3, 7-Cl, etc.; R2 = CH(CH3)2, cyclopentyl, 2-(thiophen-2-yl)ethyl, etc.; R3 = Ph, naphthalen-2-yl, 1-methyl-1H-pyrrol-2-yl, etc.; R4 = 4-H3CC6H4, biphen-4-yl, 2-pyridyl, etc.] through a novel oxidative 5-exo-dig cyclization-ketonization cascade of 2-aminobenzimidazole II [R1 = 5-CH3, 5-C(O)OCH3, 6-Cl, etc.], aldehyde R3CHO and terminal alkyne R4CCH has been explored under aerobic conditions. The reaction proceeds through copper-catalyzed addition of terminal alkynes to imines derived from 2-aminobenzimidazole with aldehyde followed by intramol. cyclization. The atm. mol. oxygen acts as an oxygen source for the newly formed carbonyl group in the final product I. In the experiment, the researchers used Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Recommanded Product: Methyl 4-fluoro-3-nitrobenzoate)

Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Recommanded Product: Methyl 4-fluoro-3-nitrobenzoateMethyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics