Month: October 2022

Related Products of 14660-52-7In 2020 ,《Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer》 appeared in European Journal of Medicinal Chemistry. The author of the article were Yao, Dahong; Li, Chenyang; Jiang, Jin; Huang, Jian; Wang, Jinhui; He, Zhendan; Zhang, Jin. The article conveys some information:

The dysfunction of histone deacetylase (HDACs) is closely related to tumorigenesis and development, which has been emerged as an attractive drug design target for cancer therapy. In the present study, a series of novel HDAC inhibitors using a substituted quinazoline as the capping group and attaching 3,5-dimethylbenyl as a potential metabolic site protector have been designed and synthesized. Compounds I and II demonstrated potent HDAC inhibitory activities and anti-proliferative effects against MDA-MB-231 cells. In addition, I and II both could significantly increase the acetylation level of intracellular proteins, especially in α-Tubulin and HSP90. Compounds I and II displayed a slight different anti-tumor mechanism, I mainly induced apoptosis while II induced obviously ER-Stress. Furthermore, I and II both induced autophagy and migration inhibition. In pharmacokinetics assay, I showed a significant improvement of pharmacokinetic profile for oral administration. Addnl., I presented more potent anti-proliferation and anti-migration activity than SAHA in zebrafish MDA-MB-231 cell line-derived xenograft model. Together, these results demonstrate that I is a novel oral HDAC inhibitor with a potential capacity of treating breast cancer. The results came from multiple reactions, including the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7Related Products of 14660-52-7)

Ethyl 5-bromovalerate(cas: 14660-52-7) 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 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

HPLC of Formula: 2969-81-5In 2022 ,《Synthesis of a cellulose dissolving liquid zwitterion from general and low-cost reagents》 appeared in Cellulose (Dordrecht, Netherlands). The author of the article were Sharma, Gyanendra; Kato, Yui; Hachisu, Ayumi; Ishibashi, Kojiro; Ninomiya, Kazuaki; Takahashi, Kenji; Hirata, Eishu; Kuroda, Kosuke. The article conveys some information:

A carboxylate-type liquid zwitterion, OE2imC3C, has been recently reported as a unique solvent as a class of ionic liquids with distinctive properties and functions such as cellulose dissolution ability and low toxicity to fermentative microoganisms. Therefore, OE2imC3C first enabled successive conversion of biomass to bioethanol in the same reaction pot. However, the reagent, 1-bromo-2-(2-methoxyethoxy)ethane, used for OE2imC3C synthesis is expensive and sometimes out of production and thus prevents its industrialization. Here we synthesized OE2imC3C from general and low-cost reagents. We also confirmed that the present OE2imC3C maintained the distinctive properties and functions because previous literature indicates synthetic procedures affect the properties. The low toxicity and cellulose dissolution ability of the OE2imC3C synthesized in this study were equivalent to those of conventional OE2imC3C. In addition, OE2imC3C is known to have ability to cryopreserve mammalian cells and the OE2imC3C synthesized in this study exhibited the ability. In the experimental materials used by the author, we found Ethyl 4-bromobutyrate(cas: 2969-81-5HPLC of Formula: 2969-81-5)

Ethyl 4-bromobutyrate(cas: 2969-81-5) 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.HPLC of Formula: 2969-81-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthetic Route of C7H13BrO2In 2021 ,《Hydrazone exchange: a viable route for the solid-tethered synthesis of [2]rotaxanes》 was published in New Journal of Chemistry. The article was written by Da Silva Rodrigues, Rafael; Luis, Ena T.; Marshall, David L.; McMurtrie, John C.; Mullen, Kathleen M.. The article contains the following contents:

Building on the success of other dynamic covalent synthetic methods, hydrazone exchange as a strategy to improve the formation of rotaxanes in solution and on solid surfaces were presented. Solution-state analogs containing naphthalenediimide (NDI) or bipyridinium motifs and 1,5-dinaphtho[38]crown-10 were initially prepared to establish ideal conditions for maintaining thermal equilibrium throughout the exchange reaction. Solid-state rotaxanes were synthesized on hydrazide-functionalised TentaGel polymer resins and analyzed with HR MAS 1H NMR spectroscopy. Surface rotaxane functionalisation of 80% was achieved for the NDI rotaxane, which was significantly higher than previously reported with either dynamic covalent or traditional irreversible synthetic strategies.Ethyl 5-bromovalerate(cas: 14660-52-7Synthetic Route of C7H13BrO2) was used in this study.

Ethyl 5-bromovalerate(cas: 14660-52-7) 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.Synthetic Route of C7H13BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Category: bromides-buliding-blocksIn 2022 ,《Soft Alloys Constructed with Distinct Mesoatoms via Self-Sorting Assembly of Giant Shape Amphiphiles》 was published in Angewandte Chemie, International Edition. The article was written by Wang, Yicong; Huang, Jiahao; Yan, Xiao-Yun; Lei, Huanyu; Liu, Xian-You; Guo, Qing-Yun; Liu, Yuchu; Liu, Tong; Huang, Mingjun; Bian, Fenggang; Su, Zebin; Cheng, Stephen Z. D.. The article contains the following contents:

The packing structures of spherical motifs affect the properties of resultant condensed materials such as in metal alloys. Inspired by the classic metallurgy, developing complex alloy-like packing phases in soft matter (also called “”soft alloys””) is promising for the next-generation superlattice engineering. Nevertheless, the formation of many alloy-like phases in single-component soft matter is usually thermodynamically unfavorable and tech. challenging. Here, we utilize a novel self-sorting assembly approach to tackle this challenge in binary blends of soft matter. Two types of giant shape amphiphiles self-sort to form their discrete spherical motifs, which further simultaneously pack into alloy-like phases. Three unconventional spherical packing phases have been observed in these binary systems, including MgZn2, NaZn13, and CaCu5 phases. It′s the first time that the CaCu5 phase is exptl. observed in soft matter. This work demonstrates a general approach to constructing unconventional spherical packing phases and other complex superlattices in soft matter. The results came from multiple reactions, including the reaction of 3,5-Dibromoaniline(cas: 626-40-4Category: bromides-buliding-blocks)

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Quality Control of 3-Bromo-2-methylbenzoic acidIn 2009 ,《O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Xu, Baihua; Lv, Binhua; Feng, Yan; Xu, Ge; Du, Jiyan; Welihinda, Ajith; Sheng, Zelin; Seed, Brian; Chen, Yuanwei. The article contains the following contents:

Two series of O-spiro C-aryl glucosides were synthesized and tested for inhibition of hSGLT1 and hSGLT2. 6′-O-Spiro C-aryl glucosides exhibited potent in vitro hSGLT2 inhibitory activity but 2′-O-spiro C-aryl glucosides showed no in vitro hSGLT2 inhibitory activity at a screening concentration of 1 μM. After reading the article, we found that the author used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Quality Control of 3-Bromo-2-methylbenzoic acid)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Quality Control of 3-Bromo-2-methylbenzoic acid The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthetic Route of C7H5BrO2In 2019 ,《Design and synthesis of new norfloxacin-1,3,4-oxadiazole hybrids as antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)》 was published in European Journal of Pharmaceutical Sciences. The article was written by Guo, Yong; Xu, Ting; Bao, Chongnan; Liu, Zhiyan; Fan, Jiangping; Yang, Ruige; Qin, Shangshang. The article contains the following contents:

Toward the search of new antibacterial agents to control methicillin-resistant Staphylococcus aureus (MRSA), aclass of new norfloxacin-1,3,4-oxadiazole hybrids were designed and synthesized. Antibacterial activities againstdrug-sensitive bacteria S. aureus and clin. drug resistant isolates of MRSA were evaluated. Compound 5k exhibited excellent antibacterial activities against S. aureus (MIC: 2μg/mL) and MRSA1-3 (MIC: 0.25-1μg/mL). The time-kill kinetics demonstrated that compound 5k had an advantage over commonly used antibiotics vancomycin in killing S. aureus and MRSA. Moreover, compound 5k could inhibit the bacteria and destroy their membranes in a short time and showed very low cytotoxicity to NRK-52E cells. Some interesting structureactivity relationships (SARs) were also discussed. These results indicated that these norfloxacin-1,3,4-oxadiazole hybrids could be further developed into new antibacterial agents against MRSA. After reading the article, we found that the author used 4-Bromobenzoic acid(cas: 586-76-5Synthetic Route of C7H5BrO2)

4-Bromobenzoic acid(cas: 586-76-5) has been used to study the metabolic fate of 2-,3-and 4-bromo benzoic acids in rat hepatocytes incubation using high temperature liquid chromatography. It was used in bromine-specific detection of the metabolites of 2-,3-and 4-bromobenzoic acid in the urine and bile of rats by inductively coupled plasma mass spectrometry.Synthetic Route of C7H5BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

COA of Formula: C6H11BrO2In 2019 ,《Formulation optimization of an ephrin A2 targeted immunoliposome encapsulating reversibly modified taxane prodrugs》 was published in Journal of Controlled Release. The article was written by Huang, Zhaohua Richard; Tipparaju, Suresh Kumar; Kirpotin, Dmitri B.; Pien, Christine; Kornaga, Tad; Noble, Charles O.; Koshkaryev, Alexander; Tran, Jimmy; Kamoun, Walid S.; Drummond, Daryl C.. The article contains the following contents:

Ephrin A2 targeted immunoliposomes incorporating pH-sensitive taxane prodrugs were developed for sustained delivery of active drug to solid tumors. Here we describe the systematic formulation development and characterization of these immunoliposomes. We synthesized both paclitaxel and docetaxel prodrugs to formulate as ephrin A2-targeted liposomes stabilized in the aqueous core with sucroseoctasulfate (SOS). The optimized lipid formulation was comprised of egg-sphingomyelin, cholesterol, and polyethylene glycol distearoyl glycerol (PEG-DSG). The formulations examined had a high efficiency of prodrug encapsulation (as high as 114 mol% taxane per mol phospholipid) and subsequent stability (>3 years at 2-8°C). The taxane prodrug was stabilized with extraliposomal citric acid and subsequently loaded into liposomes containing a gradient of SOS, resulting in highly stable SOS-drug complexes being formed inside the liposome. The internal prodrug and SOS concentrations were optimized for their impact on in vivo drug release and drug degradation Cryo-electron microscope images revealed dense prodrug-SOS complex in the aqueous core of the immunoliposomes. Ephrin A2-targeted taxane liposomes exhibited sub-nanomolar (0.69 nM) apparent equilibrium dissociation constant toward the extracellular domain of the ephrin A2 receptor, long circulation half-life (8-12 h) in mouse plasma, a release rate dependent on intraliposomal drug concentration and stable long-term storage. At an equitoxic dose of 50 mg taxane/kg, ephrin A2-targeted liposomal prodrug showed greater antitumor activity than 10 mg/kg of docetaxel in A549 non-small cell lung, as well as MDA-MB-436 and SUM149 triple neg. breast cancer xenograft models. The lead mol. entered a Phase I clin. trial in patients with solid tumors (NCT03076372). In the experimental materials used by the author, we found Ethyl 4-bromobutyrate(cas: 2969-81-5COA of Formula: C6H11BrO2)

Ethyl 4-bromobutyrate(cas: 2969-81-5) 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.COA of Formula: C6H11BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《A Concise Total Synthesis of (+)-Waihoensene Guided by Quaternary Center Analysis》 was written by Peng, Cheng; Arya, Piyush; Zhou, Zhiyao; Snyder, Scott A.. Application of 1779-49-3This research focused onwaihoensene total synthesis Conia ene cyclization Pauson Khand; Conia-ene; Pauson-Khand; total synthesis; triquinanes; waihoensene. The article conveys some information:

The four contiguous all-carbon quaternary centers of waihoensene (I), coupled with the absence of any traditional reactive functional groups other than a single alkene, render it a particularly challenging synthetic target among angular triquinane natural products. Here, we show that its polycyclic frame can be assembled concisely by using a strategically chosen quaternary center to guide the formation of the other three through judiciously selected C-C bond formation reactions. Those events, which included a unique Conia-ene cyclization and a challenging Pauson-Khand reaction, afforded a 17-step synthesis of the mol. in enantioenriched form. In the experimental materials used by the author, we found Methyltriphenylphosphonium bromide(cas: 1779-49-3Application of 1779-49-3)

Methyltriphenylphosphonium bromide(cas: 1779-49-3) is a lipophilic molecule with a cation allowing for it to be used to deliver molecules to specific cell components. Also considered an antineoplastic agent.Application of 1779-49-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《An Olefinic 1,2-Boryl-Migration Enabled by Radical Addition: Construction of gem-Bis(boryl)alkanes》 was published in Angewandte Chemie, International Edition in 2019. These research results belong to Zhao, Binlin; Li, Zexian; Wu, Yixiao; Wang, Yandong; Qian, Jiasheng; Yuan, Yu; Shi, Zhuangzhi. Product Details of 401-55-8 The article mentions the following:

A series of in situ formed alkenyl diboronate complexes from alkenyl Grignard reagents (com. available or prepared from alkenyl bromides and Mg) with B2Pin2 (bis(pinacolato)diboron) react with diverse alkyl halides by a Ru photocatalyst to give various gem-bis(boryl)alkanes. Alkyl radicals add efficiently to the alkenyl diboronate complexes, and the adduct radical anions undergo radical-polar crossover, specifically, a 1,2-boryl-anion shift from boron to the α-carbon sp2 center. This transformation shows good functional-group compatibility and can serve as a powerful synthetic tool for late-stage functionalization in complex compounds Measurements of the quantum yield reveal that a radical-chain mechanism is operative in which the alkenyl diboronates acts as reductive quencher for the excited state of the photocatalyst. The experimental process involved the reaction of Ethylbromofluoroacetate(cas: 401-55-8Product Details of 401-55-8)

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.Product Details of 401-55-8

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Decarboxylative C(sp3)-O Cross-Coupling》 was published in Angewandte Chemie, International Edition in 2018. These research results belong to Mao, Runze; Balon, Jonathan; Hu, Xile. Application of 30752-31-9 The article mentions the following:

Alkyl aryl ethers are an important class of compounds in medicinal and agricultural chem. Catalytic C(sp3)-O cross-coupling of alkyl electrophiles with phenols is an unexplored disconnection strategy to the synthesis of alkyl aryl ethers, with the potential to overcome some of the major limitations of existing methods such as C(sp2)-O cross-coupling and SN2 reactions. Reported here is a tandem photoredox and copper catalysis to achieve decarboxylative C(sp3)-O coupling of alkyl N-hydroxyphthalimide (NHPI) esters with phenols under mild reaction conditions. This method was used to synthesize a diverse set of alkyl aryl ethers using readily available alkyl carboxylic acids, including many natural products and drug mols. Complementarity in scope and functional-group tolerance to existing methods was demonstrated. In the experimental materials used by the author, we found 1-Bromo-4-(cyclohexyloxy)benzene(cas: 30752-31-9Application of 30752-31-9)

1-Bromo-4-(cyclohexyloxy)benzene(cas: 30752-31-9) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Application of 30752-31-9 The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary