Tag: 100-200

The author of 《Repositioning Salirasib as a new antimalarial agent》 were Porta, Exequiel O. J.; Bofill Verdaguer, Ignasi; Perez, Consuelo; Banchio, Claudia; Ferreira de Azevedo, Mauro; Katzin, Alejandro M.; Labadie, Guillermo R.. And the article was published in MedChemComm in 2019. Related Products of 539-74-2 The author mentioned the following in the article:

Malaria is a serious tropical disease that kills thousands of people every year, mainly in Africa, due to Plasmodium falciparum infections. Salirasib is a promising cancer drug candidate that interferes with the post-translational modification of Ras. This S-farnesyl thiosalicylate inhibits isoprenylcysteine carboxyl methyltransferase (ICMT), a validated target for cancer drug development. There is a high homol. between the human and the parasite enzyme isoforms, in addition to being a druggable target. Looking to repurpose its structure as an antimalarial drug, a collection of S-substituted derivatives of thiosalicylic acid were prepared by introducing 1,2,3-triazole as a diversity entry point or by direct alkylation of the thiol. We further investigated the in vitro toxicity of FTS analogs to Plasmodium falciparum in the asexual stages and in Vero cells. An antiplasmodial activity assay was performed using a simple, high-sensitivity methodol. based on nanoluciferase (NLuc)-transfected P. falciparum parasites. The results showed that some of the analogs were active at low micromolar concentration, including Salirasib. The most potent member of the series has S-farnesyl and the 1,2,3-triazole moiety substituted with phytyl. However, the compound substituted with methyl-naphthyl shows promising physicochem. and activity values. The low cytotoxicity in eukaryotic cells of the most active analogs provided good therapeutic indexes, being starting-point candidates for future antimalarial drug development. In the experimental materials used by the author, we found Ethyl 3-bromopropanoate(cas: 539-74-2Related Products of 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Related Products of 539-74-2 Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Application In Synthesis of 1-Bromo-2-isopropylbenzeneIn 2016 ,《Microwave-assisted copper- and palladium-catalyzed Sonogashira-type coupling of aryl bromides and iodides with trimethylsilylacetylene》 was published in Tetrahedron Letters. The article was written by Lei, Yonghua; Hu, Tianhan; Wu, Xingsen; Wu, Yue; Xiang, Hua; Sun, Haopeng; You, Qidong; Zhang, Xiaojin. The article contains the following contents:

An efficient and rapid method was developed for the synthesis of 1-aryl-2-(trimethylsilyl)acetylene. Copper and palladium-catalyzed Sonogashira-type coupling of trimethylsilylacetylene and aryl bromides or iodides in the presence of triethylamine as base under microwave irradiation in acetonitrile afforded the desired 1-aryl-2-(trimethylsilyl)acetylene. The use of microwave was found to significantly improve the reaction yield and shorten the reaction time. In the experiment, the researchers used many compounds, for example, 1-Bromo-2-isopropylbenzene(cas: 7073-94-1Application In Synthesis of 1-Bromo-2-isopropylbenzene)

1-Bromo-2-isopropylbenzene(cas: 7073-94-1) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Application In Synthesis of 1-Bromo-2-isopropylbenzene Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Recommanded Product: o-BromobenzaldehydeIn 2019 ,《A nanostructured organic-inorganic hybrid material: Preparation, characterization and catalytic performance for the synthesis of N,N’-alkylidene bisamides》 was published in ChemistrySelect. The article was written by Zare, Abdolkarim; Khanivar, Roghayyeh; Irannejad-Gheshlaghchaei, Navid; Beyzavi, M. Hassan. The article contains the following contents:

A novel nanostructured mesoporous organic-inorganic hybrid material, based on dicationic ionic liquid – anchored with silica, namely nano-2-[N’,N’-dimethyl-N’-(silica-n-propyl)ethanaminium chloride]-N,N-dimethylaminium bisulfate {nano-[DSPECDA][HSO4]}, was prepared and characterized by FT-IR, energy-dispersive X-ray spectroscopy, field emission SEM, X-ray diffraction, thermal gravimetry, differential thermal gravimetric, DTA and adsorption/desorption porosimetry (BET, Langmuir, adsorption/desorption isotherm, BJH and t-plot) methods. Thereafter, the nanomaterial was utilized as a highly effectual, heterogeneous and recyclable nanocatalyst for the synthesis of N,N’-alkylidene bisamides RCONHCH(Ar)NHCOR [R = Me, Ph, Ar = Ph, 4-MeC6H4, 2-BrC6H4, 4-O2NC6H4, etc.] via the condensation reaction of benzaldehydes (1 equivalent) with primary amides (2 equivalent) under solvent-free conditions. The reaction results were better compared with the literature in terms of two or more of these factors: turnover frequency (TOF), yield, temperature, time and the reaction media. The experimental process involved the reaction of o-Bromobenzaldehyde(cas: 6630-33-7Recommanded Product: o-Bromobenzaldehyde)

o-Bromobenzaldehyde(cas: 6630-33-7) is used in L-threonine aldolase-catalyzed enantio/diastereoselective aldol reactions.Recommanded Product: o-BromobenzaldehydeIt is also used in L-threonine aldolase-catalyzed enantio and diastereoselective aldol reactions. Further, it reacts with trichloromethane to prepare 1-(2-bromo-phenyl)-2,2,2-trichloro-ethanol.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Zhifang; Li, Zuojie; Du, Tao; Chen, Yan; Wang, Qingpeng; Li, Guoshuai; Liu, Min; Zhang, Ning; Li, Dacheng; Han, Jun published an article in 2021. The article was titled 《Design, synthesis and biological evaluation of dihydro-2-quinolone platinum(IV) hybrids as antitumor agents displaying mitochondria injury and DNA damage mechanism》, and you may find the article in Dalton Transactions.Related Products of 3395-91-3 The information in the text is summarized as follows:

The design of novel platinum(IV) complexes with mitochondria injury competence, besides the DNA damage mechanism, is a promising way to develop new platinum drugs. Herein, dihydro-2-quinolone (DHQLO) as a mitocan was incorporated into the platinum(IV) system for the first time to prepare a new series of DHQLO platinum(IV) compounds Complex 1b could effectively inhibit the proliferation of tumor cells in vitro and in vivo. It accumulated at higher levels in both whole cells and DNA, and easily underwent intercellular reduction to release platinum(II) and DHQLO moieties. The released platinum(II) complex caused serious DNA damage by covalent conjunction with the DNA duplex, and remarkably increased the expression of the γ-H2AX protein. Moreover, 1b also caused serious mitochondria injury to induce mitochondrial membrane depolarization and increase ROS generation. Such actions upon DNA and mitochondria activate the p53 apoptotic pathway synergetically in tumor cells by upregulating the protein p53 and apoptotic proteins caspase9 and caspase3, which efficiently promoted the apoptotic death of tumor cells. Compound 1b with such synergic mechanism exhibited great potential in reversing cisplatin resistance and improving antitumor efficacies. After reading the article, we found that the author used Methyl 3-bromopropanoate(cas: 3395-91-3Related Products of 3395-91-3)

Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Related Products of 3395-91-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Tailored Polymers with Complement Activation Ability To Improve Antitumor Immunity》 were Li, Chenxi; Lu, Yue; Chen, Qing; Hu, Haiyang; Zhao, Xiuli; Qiao, Mingxi; Chen, Dawei. And the article was published in Molecular Pharmaceutics in 2019. Safety of Ethyl 3-bromopropanoate The author mentioned the following in the article:

The complement system plays an important role in host innate immunity, and its activation can be exploited as a potential strategy for vaccine adjuvants. Herein, a pH-responsive micellar vaccine platform (COOH-NPs) was developed using a carboxyl-modified diblock copolymer of poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) (COOH-PEOz-PLA). The copolymer self-assembled into micelles with hydroxyl groups shielding on the surface, which activated the complement system for the enhanced immune responses. Compared with the control nanoparticles (OCH3-NPs), COOH-NPs significantly enhanced lymph node-resident dendritic cell maturation, antigen-specific IgG production, antigen-specific CD4+ and CD8+ T-cell activation, and the amount of memory T-cell generation in vivo. Furthermore, immunization with COOH-NPs/OVA in E.G7-OVA tumor-bearing mice not only remarkably inhibited tumor growth but also prolonged the survival of tumor-bearing mice. These results indicated that COOH-NPs with the capability of complement activation efficiently boosted the immune responses for the antitumor effect. The study demonstrated the significance of taking advantage of a complement-activating vaccine platform for cancer immunotherapy.Ethyl 3-bromopropanoate(cas: 539-74-2Safety of Ethyl 3-bromopropanoate) was used in this study.

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Safety of Ethyl 3-bromopropanoateSome of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2019,Nature Communications included an article by He, Zhi-Tao; Hartwig, John F.. SDS of cas: 7073-94-1. The article was titled 《Palladium-catalyzed α-arylation for the addition of small rings to aromatic compounds》. The information in the text is summarized as follows:

A generally applicable approach to attach small rings to a wide range of aromatic compounds by palladium-catalyzed α-arylation of cyclopropyl, cyclobutyl and azetidinyl esters was reported. The direct α-arylation of cyclopropyl esters and cyclobutyl esters was achieved in high yield by ensuring that rate of coupling exceeded rate of Claisen condensation. The α-arylation of azetidines was achieved without ring opening of strained saturated heterocycle by conducting reactions with an azetidine derivative bearing a benzyl protecting group on nitrogen. Mechanistic studies showed that α-arylation of small rings was challenging because of the weak acidity of α C-H bond (cyclopropanes), strong sensitivity of strained esters to Claisen condensation (cyclobutatanes), or facile decomposition of enolates (azetidinyl esters). In the experiment, the researchers used 1-Bromo-2-isopropylbenzene(cas: 7073-94-1SDS of cas: 7073-94-1)

1-Bromo-2-isopropylbenzene(cas: 7073-94-1) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. SDS of cas: 7073-94-1 Alkyl bromides are mainly used as alkylating agents and also find application as a solvent to extract oil from seeds and wool.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2016,Gildner, Peter G.; DeAngelis, Andrew; Colacot, Thomas J. published 《Palladium-Catalyzed N-Arylation of Cyclopropylamines》.Organic Letters published the findings.Computed Properties of C9H11Br The information in the text is summarized as follows:

A general method has been developed for the previously challenging arylation of cyclopropylamine and N-arylcyclopropylamines. Highly active, air-stable, and com. available R-allylpalladium precatalysts provide access to a wide range of (hetero)arylated cyclopropylanilines in high yields. Precatalysts [(tBuBrettPhos)Pd(allyl)]OTf and [(BrettPhos)Pd(crotyl)]OTf deliver monoarylated products, while (PtBu3)Pd(crotyl)Cl is suited for preparing unsym. diarylated products. The developed conditions tolerate a range of functional groups and heterocycles, allowing access to an array of arylated cyclopropylamines, a motif present in prominent drug mols.1-Bromo-2-isopropylbenzene(cas: 7073-94-1Computed Properties of C9H11Br) was used in this study.

1-Bromo-2-isopropylbenzene(cas: 7073-94-1) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. Computed Properties of C9H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Mazzarella, Daniele; Magagnano, Giandomenico; Schweitzer-Chaput, Bertrand; Melchiorre, Paolo published an article in ACS Catalysis. The title of the article was 《Photochemical Organocatalytic Borylation of Alkyl Chlorides, Bromides, and Sulfonates》.Recommanded Product: Ethylbromofluoroacetate The author mentioned the following in the article:

Reported herein is a photochem. strategy for the borylation of alkyl halides using bis(catecholato)diboron as the boron source. This method exploits the ability of a nucleophilic dithiocarbonyl anion organocatalyst to generate radicals via an SN2-based photochem. catalytic mechanism, which is not reliant on the redox properties of the substrates. Therefore, it grants access to alkyl boronic esters from readily available but difficult-to-reduce electrophiles, including benzylic and allylic chlorides, bromides, and mesylates, which were inert to or unsuitable for previously reported metal-free borylation protocols. In addition to this study using Ethylbromofluoroacetate, there are many other studies that have used Ethylbromofluoroacetate(cas: 401-55-8Recommanded Product: Ethylbromofluoroacetate) was used in this study.

Ethylbromofluoroacetate(cas: 401-55-8) is a member of organofluorine compounds. Organofluorine compounds, which have carbon-fluorine bonds, show unique features such as high thermal and chemical stability, high surface activity, no light-absorbing ability, high pharmacological effect, and so on. Owing to their specific characters, they are indispensable chemicals for industry and our daily lives.Recommanded Product: Ethylbromofluoroacetate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Formula: C4H6BrFO2On October 3, 2019 ,《Copper-catalyzed remote C-H monofluoromethylation of 8-aminoquinolines with dimethyl phosphonate as reductant》 was published in Tetrahedron Letters. The article was written by Han, Shuaijun; Wu, Qingsong; Mele, Lucas; Ding, Licheng; Li, Jingya; Zou, Dapeng; Wu, Yusheng; Wu, Yangjie. The article contains the following contents:

A simple and efficient copper-catalyzed monofluoromethylation of 8-aminoquinolines with 2-bromo-2-fluoroacetate was described with HPO(OMe)2 (di-Me phosphonate) as reductant. The reaction tolerated a variety of quinoline amides and monofluoroalkyl bromides. Significant advantages of this protocol include synthetic convenience and high reaction efficiency. The experimental process involved the reaction of Ethylbromofluoroacetate(cas: 401-55-8Formula: C4H6BrFO2)

Ethylbromofluoroacetate(cas: 401-55-8) is a member of organofluorine compounds. Organofluorine compounds, which have carbon-fluorine bonds, show unique features such as high thermal and chemical stability, high surface activity, no light-absorbing ability, high pharmacological effect, and so on. Owing to their specific characters, they are indispensable chemicals for industry and our daily lives.Formula: C4H6BrFO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Synthesis, Structural Characterization, and Coordination Chemistry of (Trineopentylphosphine)palladium(aryl)bromide Dimer Complexes ([(Np3P)Pd(Ar)Br]2)》 was written by Hu, Huaiyuan; Vasiliu, Monica; Stein, Trent H.; Qu, Fengrui; Gerlach, Deidra L.; Dixon, David A.; Shaughnessy, Kevin H.. Application In Synthesis of 1-Bromo-2-isopropylbenzeneThis research focused ontrineopentylphosphine palladium aryl bromide dimer preparation crystal mol structure; cross coupling Buchwald Hartwig amination trineopentylphosphine palladium aryl bromide; binding equilibrium pyridine trineopentylphosphine palladium aryl bromide dimer. The article conveys some information:

A series of [(PNp3)Pd(Ar)Br]2 complexes (PNp3 = trineopentylphosphine, Ar = 4-tolyl, 4-tert-butylphenyl, 2-tolyl, 4-methoxy-2-methylphenyl, 2-isopropylphenyl, and 2,6-dimethylphenyl) were synthesized and structurally characterized by x-ray crystallog. and d. functional theory optimized structures. The trineopentylphosphine ligand is able to accommodate coordination of other sterically demanding ligands through changes in its conformation. These conformational changes can be seen in changes in percent buried volume of the PNp3 ligand. The binding equilibrium of the [(PNp3)Pd(Ar)Br]2 complexes with pyridine derivatives were determined exptl. and analyzed computationally. The binding equilibrium are sensitive to the steric demand of the pyridine ligand and less sensitive to the steric demand of the aryl ligand on palladium. In contrast to previous studies, the binding equilibrium do not correlate with pyridine basicity. The binding equilibrium results are relevant to fundamental ligand coordination steps in cross-coupling reactions, such as Buchwald-Hartwig aminations. X-ray crystal structures of [(PNp3)Pd(Ar)Br]2 (PNp3 = trineopentylphosphine) are reported and compared to DFT-optimized geometries. The PNp3 ligand is highly flexible, allowing coordination of hindered aryl ligands. Binding equilibrium with pyridine depend primarily on the steric demand of the pyridine and the aryl ligand, whereas pyridine basicity is not a major factor. In the experiment, the researchers used many compounds, for example, 1-Bromo-2-isopropylbenzene(cas: 7073-94-1Application In Synthesis of 1-Bromo-2-isopropylbenzene)

1-Bromo-2-isopropylbenzene(cas: 7073-94-1) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Application In Synthesis of 1-Bromo-2-isopropylbenzene Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary