Tag: 200-300

On September 16, 2016, Zhang, Ziqian; Li, Yi; He, Haihong; Qian, Xuhong; Yang, Youjun published an article.SDS of cas: 99-60-5 The title of the article was Mild Chemotriggered Generation of a Fluorophore-Tethered Diazoalkane Species via Smiles Rearrangement. And the article contained the following:

Nitrosamino naphthalenedicarboximide I and a related disulfide underwent Smiles rearrangement in the presence of nucleophiles to generate diazo compounds in situ under mild conditions (in aqueous buffer or MeCN at ambient temperature); reaction with nucleophiles such as carboxylic acids RCO2H [R = Me, i-Pr, Me(CH2)10, (E,E)-MeCH:CHCH:CH, Me2C:CH, 1-adamantyl, Ph, 3-HOC6H4, 2-HOC6H4, 2-Ph2PC6H4, 4-MeC6H4, 4-BrC6H4, 4-O2NC6H4, 2-Cl-4-O2NC6H3, 4-Et2NC6H4, 1-naphthyl] or dimethylamine or activation with glutathione yielded fluorescent products such as acyloxyethylthio naphthalenedicarboximides II [R = Me, i-Pr, Me(CH2)10, (E,E)-MeCH:CHCH:CH, Me2C:CH, 1-adamantyl, Ph, 3-HOC6H4, 2-HOC6H4, 2-Ph2PC6H4, 4-MeC6H4, 4-BrC6H4, 4-O2NC6H4, 2-Cl-4-O2NC6H3, 4-Et2NC6H4, 1-naphthyl] in 16-45% yields. The structure of I was determined by X-ray crystallog. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).SDS of cas: 99-60-5

The Article related to nitrosamino naphthalenedicarboximide preparation rearrangement nucleophile, acyloxyethylthio naphthalenedicarboximide preparation fluorescence, diazo compound formation smiles rearrangement nitrosamino naphthalenedicarboximide, carboxylic acid reaction in situ generated diazo compound, acetylthioethyl nitrosamino naphthalenedicarboximide mol crystal structure and other aspects.SDS of cas: 99-60-5

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

On April 16, 2021, Xu, Changming; Qi, Yinsheng; Yang, Xinshuang; Li, Xiangfan; Li, Zhenpeng; Bai, Lei published an article.HPLC of Formula: 14602-86-9 The title of the article was Development of C2-Symmetric Chiral Spirocyclic Phase-Transfer Catalysts: Synthesis and Application to Asymmetric Alkylation of Glycinate Schiff Base. And the article contained the following:

A class of C2-sym. chiral spirocyclic phase-transfer catalysts based on the tetramethyl-1,1′-spirobiindane scaffold such as I·Br- was synthesized from com. available bisphenol A in 12 steps in 22-25% total yields; the scaffold features a more rigid and stable backbone and smaller dihedral angles and can be easily modified. These catalysts show high catalytic performance in the asym. alkylation of tert-Bu glycinate Schiff base Ph2C:NCH2CO2t-Bu at only 2 mol % catalyst loading, giving nonracemic protected α-amino acid esters such as (R)-Ph2C:NCH(CH2Ph)CO2t-Bu in up to 92% yield and 98% ee. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).HPLC of Formula: 14602-86-9

The Article related to spirobiindanoazocinium nonracemic preparation catalyst enantioselective phase transfer alkylation, diphenylmethyleneamino ester enantioselective preparation, nonracemic spirobiindanoazocinium bromide enantioselective phase transfer alkylation catalyst, alkyl bromide enantioselective alkylation diphenylmethyleneamino ester spirobiindanoazocinium catalyst and other aspects.HPLC of Formula: 14602-86-9

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

On September 2, 2011, Curti, Claudio; Battistini, Lucia; Sartori, Andrea; Lodola, Alessio; Mor, Marco; Rassu, Gloria; Pelosi, Giorgio; Zanardi, Franca; Casiraghi, Giovanni published an article.Reference of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate The title of the article was Catalytic, Asymmetric Hypervinylogous Mukaiyama Aldol Reactions of Extended Furan-Based Silyl Enolates. And the article contained the following:

Vinyl, butadienyl, and hexatrienyl siloxyfurans such as I (TBS = tert-butyldimethylsilyl) are prepared; in the presence of silicon tetrachloride and nonracemic bis(dinaphthodiazaphosphepine) II, I undergo regioselective, stereoselective, and enantioselective vinylogous Mukaiyama aldol addition reactions with aryl aldehydes to yield nonracemic hydroxyalkylidenefuranones such as III in 42-92% yields, in 55:45->95:5 olefin stereoselectivities, and in 89:11->99:1 er. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Reference of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate

The Article related to vinyl butadienyl hexatrienyl siloxyfuran preparation regioselective stereoselective aldol addition, hydroxyalkylidenefuranone regioselective stereoselective preparation, silicon chloride dinaphthodiazaphosphepine catalyst regioselective enantioselective hypervinylogous aldol addition, vinylogous mukaiyama aldol addition vinyl siloxyfuran aryl aldehyde and other aspects.Reference of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate

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

On April 1, 2021, Xiong, Shili; Wang, Nan; Liu, Chao; Shen, Huaxing; Qu, Zengqiang; Zhu, Lijun; Bai, Xiaosong; Hu, Hong-gang; Cong, Wei; Zhao, Liang published an article.SDS of cas: 98946-18-0 The title of the article was Design, synthesis, and anti-tumor activities of novel Brevinin-1BYa peptidomimetics. And the article contained the following:

Brevinin-1BYa is an amphibian skin-derived peptide that exhibits promising anti-microbial activity against gram-pos. and -neg. bacteria. However, the anti-tumor activity of Brevinin-1BYa remains unclear, and, more importantly, its therapeutic application is limited owing to its poor protease and reduction stability. In this study, a series of novel Brevinin-1BYa derivatives, including O-linked N-acetyl-glucosamine glyclopeptides and disulfide bond mimetics, were designed and synthesized. Addnl., their anti-tumor activity against human prostate cancer cell line C4-2B, human NSCLC cell line A549 (adenocarcinoma), and human hepatoma cells line HuH-7 was investigated. Among these, the thioether bridge substituted peptidomimetic Brevinin-1BYa-3 displayed improved reduction stability, more stable secondary structure, greater protease stability, and increased anti-tumor activity compared with the original peptide, rendering it a promising leading compound for drug development, particularly for applications against malignant tumors. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).SDS of cas: 98946-18-0

The Article related to cyclic peptide synthesis glycopeptide antitumor structure activity drug design, homoserine bromination solid phase synthesis peptide coupling oxidative cyclization, peptidomimetic click chem azide alkyne cycloaddition copper catalyst lactamization, secondary structure enzymic stability peptide folding hemolysis, anti-tumor activity, brevinin-1bya and other aspects.SDS of cas: 98946-18-0

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

On January 1, 2010, Gonzalez, Ana Z.; Toste, F. Dean published an article.Recommanded Product: 14602-86-9 The title of the article was Gold(I)-Catalyzed Enantioselective [4+2]-Cycloaddition of Allene-dienes. And the article contained the following:

An enantioselective gold(I)-catalyzed intramol. [4+2]-cycloaddition of allenes and dienes is reported. The reactions allow for the asym. synthesis of trans-hexahydroindenes and pyrrolidine products using C3-sym. phosphitegold(I) and ortho-arylphosphoramiditegold(I) complexes as catalysts, resp. The x-ray crystal structures of two phosphoramiditegold(I) complexes and two C3-sym. phosphitegold(I) complexes are reported. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Recommanded Product: 14602-86-9

The Article related to phosphite gold axially chiral catalyst preparation crystal mol structure, phosphoramidite gold axially chiral catalyst preparation crystal mol structure, allene diene substrate preparation chiral gold catalyst intramol cycloaddition, hexahydroindene derivative stereoselective preparation, pyrrolidine fused derivative stereoselective preparation and other aspects.Recommanded Product: 14602-86-9

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

On December 1, 2019, Wu, Renbo; Liu, Song; Liu, Yajing; Sun, Yuli; Cheng, Xuebo; Huang, Yong; Yang, Zequn; Wu, Zehui published an article.Synthetic Route of 98946-18-0 The title of the article was Synthesis and biological evaluation of [18F](2S,4S)4-(3-fluoropropyl) arginine as a tumor imaging agent. And the article contained the following:

Designing novel 18F-labeled amino acid derivatives for targeted amino acid transporters is an attractive strategy for the development of therapeutic and diagnostic agents for cancer therapy. In this work, we have developed a novel 3-fluoropropyl analog of arginine, namely, (2S,4S)4-[18F]FPArg, [18F]1, to be used as a probe for studying arginine metabolism Optically pure and labeled with 18F and 19F, (2S,4S)4-(3-fluoropropyl)arginine was synthesized and isolated in high radiochem. purity (>95%). In vitro uptake assays in human MCF-7 cells revealed that [18F]1 enters cells mainly via sodium-independent cationic amino acid transporters and was inhibited >62% by arginine. [18F]1 showed a high cellular uptake of 7.3 ± 0.24% and 6.07 ± 0.3% uptake/100 mg protein after incubation in MCF-7 and MDA-MB-231 cells for 120 min, resp. In vivo biodistribution studies demonstrated that [18F]1 provided high tumor uptake and high tumor to muscle ratios (5:1 at the 30 and 60 min time points). In vivo PET imaging studies demonstrated tumor-specific uptake in nude mice bearing MCF-7 breast tumors with an excellent tumor-to-muscle ratio. These results suggest that [18F]1 is a promising tracer for clin. breast cancer imaging and may be used to diagnose and monitor diseases that are associated with arginine metabolism The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Synthetic Route of 98946-18-0

The Article related to fluoropropyl arginine 18f isotope synthesis tumor imaging agent pet, amino acid uptake breast tumor biodistribution metabolism diagnostic agent, pyrazole carboxamidine guanidinylation mitsunobu reaction protection coupling fluorination reduction, phase transfer catalyst steric hindrance, arginine, breast cancer, cationic amino acid transporter and other aspects.Synthetic Route of 98946-18-0

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

Schlauderer, Florian; Lammens, Katja; Nagel, Daniel; Vincendeau, Michelle; Eitelhuber, Andrea C.; Verhelst, Steven H. L.; Kling, Dale; Chrusciel, Al; Ruland, Juergen; Krappmann, Daniel; Hopfner, Karl-Peter published an article in 2013, the title of the article was Structural Analysis of Phenothiazine Derivatives as Allosteric Inhibitors of the MALT1 Paracaspase.Category: chlorides-buliding-blocks And the article contains the following content:

The authors report the crystal structure of ligand-free dimeric human MALT1casp-Ig3 in complex with the tricyclic phenothiazine derivative thioridazine. Unexpectedly, the structure reveals that the inhibitor binds in a pocket located on the opposite to the caspase active site, in the interface between the caspase domain and the Ig3 domain connecting helix α1Ig3 of MALT1. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Category: chlorides-buliding-blocks

The Article related to phenothiazine malt1 paracaspase allosteric inhibitor crystal mol structure design, antitumor multiple sclerosis enzyme inhibitor design phenothiazine derivative prepare, enantiomer resolution phenothiazine malt1 paracaspase allosteric inhibitor mol docking, cancer, inhibitors, medicinal chemistry, multiple sclerosis, thioridazine and other aspects.Category: chlorides-buliding-blocks

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

On March 8, 2018, Lopez-Tapia, Francisco; Brotherton-Pleiss, Christine; Yue, Peibin; Murakami, Heide; Costa Araujo, Ana Carolina; Reis dos Santos, Bruna; Ichinotsubo, Erin; Rabkin, Anna; Shah, Raj; Lantz, Megan; Chen, Suzie; Tius, Marcus A.; Turkson, James published an article.Synthetic Route of 98946-18-0 The title of the article was Linker variation and structure-activity relationship analysis of carboxylic acid-based small molecule STAT3 inhibitors. And the article contained the following:

The mol. determinants for the activities of the reported benzoic acid (SH4-54), salicylic acid (BP-1-102), and benzohydroxamic acid (SH5-07)-based STAT3 inhibitors were investigated to design optimized analogs. All three leads are based on an N-methylglycinamide scaffold, with its two amine groups condensed with three different functionalities. The three functionalities and the CH2 group of the glycinamide scaffold were sep. modified. The replacement of the pentafluorobenzene or cyclohexylbenzene, or replacing the benzene ring of the aromatic carboxylic or hydroxamic acid motif with heterocyclic components (containing nitrogen and oxygen elements) all decreased potency. Notably, the Ala-linker analogs, (I) (R1 = H and OH), and the Pro-based derivative (II) (X = CH2), all with (R)-configuration at the chiral center, had improved inhibitory activity and selectivity against STAT3 DNA-binding activity in vitro, with IC50 of 3.0 ± 0.9, 1.80 ± 0.94, and 2.4 ± 0.2 μM, resp. Compounds I and II and other analogs inhibited constitutive STAT3 phosphorylation and activation in human breast cancer and melanoma lines, and blocked tumor cell viability, growth, colony formation, and migration in vitro. Pro-based analog, II (X = O)(sodium salt), with a relatively polar tetrahydropyranyl (THP) ring, instead of the cyclohexyl, showed improved permeability. In general, the (R)-configuration Pro-based analogs showed the overall best profile, including physicochem. properties (e.g., microsomal metabolic stability, Caco-2 permeability), and in particular, II (X = CH2) showed improved tumor-cell specificity. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Synthetic Route of 98946-18-0

The Article related to amino acid sulfonamide synthesis stat3 inhibitor structure activity pharmacokinetic, antitumor agent metabolic stability permeability stat3 dna binding inhibitor, alanine proline sulfonylation pentafluorobenzene cyclohexylbenzene acylation amination reductive alkylation, sulfonamide methylglycinamide drug design mechanism action and other aspects.Synthetic Route of 98946-18-0

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

On March 8, 2018, Lopez-Tapia, Francisco; Brotherton-Pleiss, Christine; Yue, Peibin; Murakami, Heide; Costa Araujo, Ana Carolina; Reis dos Santos, Bruna; Ichinotsubo, Erin; Rabkin, Anna; Shah, Raj; Lantz, Megan; Chen, Suzie; Tius, Marcus A.; Turkson, James published an article.Computed Properties of 99-60-5 The title of the article was Linker variation and structure-activity relationship analysis of carboxylic acid-based small molecule STAT3 inhibitors. And the article contained the following:

The mol. determinants for the activities of the reported benzoic acid (SH4-54), salicylic acid (BP-1-102), and benzohydroxamic acid (SH5-07)-based STAT3 inhibitors were investigated to design optimized analogs. All three leads are based on an N-methylglycinamide scaffold, with its two amine groups condensed with three different functionalities. The three functionalities and the CH2 group of the glycinamide scaffold were sep. modified. The replacement of the pentafluorobenzene or cyclohexylbenzene, or replacing the benzene ring of the aromatic carboxylic or hydroxamic acid motif with heterocyclic components (containing nitrogen and oxygen elements) all decreased potency. Notably, the Ala-linker analogs, (I) (R1 = H and OH), and the Pro-based derivative (II) (X = CH2), all with (R)-configuration at the chiral center, had improved inhibitory activity and selectivity against STAT3 DNA-binding activity in vitro, with IC50 of 3.0 ± 0.9, 1.80 ± 0.94, and 2.4 ± 0.2 μM, resp. Compounds I and II and other analogs inhibited constitutive STAT3 phosphorylation and activation in human breast cancer and melanoma lines, and blocked tumor cell viability, growth, colony formation, and migration in vitro. Pro-based analog, II (X = O)(sodium salt), with a relatively polar tetrahydropyranyl (THP) ring, instead of the cyclohexyl, showed improved permeability. In general, the (R)-configuration Pro-based analogs showed the overall best profile, including physicochem. properties (e.g., microsomal metabolic stability, Caco-2 permeability), and in particular, II (X = CH2) showed improved tumor-cell specificity. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Computed Properties of 99-60-5

The Article related to amino acid sulfonamide synthesis stat3 inhibitor structure activity pharmacokinetic, antitumor agent metabolic stability permeability stat3 dna binding inhibitor, alanine proline sulfonylation pentafluorobenzene cyclohexylbenzene acylation amination reductive alkylation, sulfonamide methylglycinamide drug design mechanism action and other aspects.Computed Properties of 99-60-5

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

On March 4, 2020, Kayser, Silke; Temperini, Piero; Poulie, Christian B. M.; Staudt, Markus; Nielsen, Birgitte; Pickering, Darryl S.; Bunch, Lennart published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was A Diversity Oriented Synthesis Approach to New 2,3-trans-Substituted L-Proline Analogs as Potential Ligands for the Ionotropic Glutamate Receptors. And the article contained the following:

Discovery of chem. tools for the ionotropic glutamate receptors continues to be a challenging task. Herein we report a diversity-oriented approach to new 2,3-trans-L-proline analogs whereby we study how the spatial orientation of the distal carboxylate group influence on binding affinity and receptor class and subtype selectivity. In total 10 new analogs were synthesized and the 14 stereoisomers characterized in binding assays at native rat ionotropic glutamate receptors, and at cloned human homomeric kainic acid (KA) receptor subtypes GluK1-3. The study identified isoxazole analogs (I) (R1 = OH, CO2H), which displayed selectivity in binding at native N-methyl-D-aspartate (NMDA) receptors over native α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and KA receptors, in the high nanomolar to low micromolar range. Furthermore, analogs (II) showed preference in binding affinity for GluK3 over GluK1,2. Finally, analog (III) displayed high nanomolar affinity for native NMDA receptors as well as for homomeric GluK3 receptors. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to proline analog enantioselective diastereoselective synthesis ka nmda ampa ligand, ka nmda ampa ionotropic glutamate receptor binding structure activity, aryl proline trans cis epimerization coupling aminoquinoline alkynylation protection, diversity-oriented synthesis, ionotropic glutamate receptors, proline analogs, sar study and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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