Category: 98946-18-0

Brodrecht, Martin; Herr, Kevin; Bothe, Sarah; de Oliveira, Marcos Jr.; Gutmann, Torsten; Buntkowsky, Gerd published an article in 2019, the title of the article was Efficient building blocks for solid-phase peptide synthesis of spin labeled peptides for electron paramagnetic resonance and dynamic nuclear polarization applications.Formula: C6H10Cl3NO And the article contains the following content:

Specific spin labeling allows the site-selective investigation of biomols. by EPR and DNP enhanced NMR spectroscopy. A novel spin labeling strategy for com. available Fmoc-amino (Fmoc = 9-fluorenylmethoxycarbonyl) acids is developed. In this approach, the PROXYL spin label is covalently attached to the hydroxyl side chain of three amino acids hydroxyproline (Hyp), serine (Ser) and tyrosine (Tyr) by a simple three-step synthesis route. The obtained PROXYL containing building-blocks are N-terminally protected by the Fmoc-protection group, which makes them applicable for the use in solid-phase peptide synthesis (SPPS). This approach allows the insertion of the spin label at any desired position during SPPS, which makes it more versatile than the widely used post synthetic spin labeling strategies. For the final building-blocks, the radical activity is proven by EPR. DNP enhanced solid-state NMR experiments employing these building-blocks in a TCE solution show enhancement factors of up to 26 for 1H and 13C (1H→13C cross-polarization). To proof the viability of the presented building-blocks for insertion of the spin label during SPPS the penta-peptide Acetyl-Gly-Ser(PROXYL)-Gly-Gly-Gly was synthesized employing the spin labeled Ser building-block. This peptide could successfully be isolated and the spin label activity proved by EPR and DNP NMR measurements, showing enhancement factors of 12.1±0.1 for 1H and 13.9±0.5 for 13C (direct polarization). The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Formula: C6H10Cl3NO

The Article related to amino acid fmoc protected spin label proxyl esr dnp, solid phase peptide synthesis spin label esr dnp nmr, epr, amino acids, hyperpolarization, solid-state nmr, spin labeling and other aspects.Formula: C6H10Cl3NO

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

Engl, Oliver D.; Saadi, Jakub; Cosimi, Elena; Wennemers, Helma published an article in 2017, the title of the article was Synthesis of Monothiomalonates – Versatile Thioester Enolate Equivalents for C-C Bond Formations.Recommanded Product: tert-Butyl trichloroacetimidate And the article contains the following content:

A method for the preparation of monothiomalonates, used as thioester enolate equivalent for stereoselective C-C bond formation, is disclosed; the method allows the thioester and ester groups and the carbon substituents to be varied. Reaction of Meldrum’s acid and 2-substituted Meldrum’s acids with arylthiols or (4-methoxyphenylthio)trimethylsilane mediated by Et3N and TMSCl in MeCN yielded malonic acid monothioesters which were isolated in most cases by extraction O-alkylation of the resulting malonic acid monothioesters with alkyl triflates or alkyl acetimidates yielded the desired monothiomalonates in 34-92% overall yields. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to monothiomalonate preparation, ring opening meldrum acid aryl thiol chlorotrimethylsilane ethylamine, alkylation malonic acid monothioester alkyl trichloroacetimidate triflate and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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

On February 16, 2018, Hawkins, Paige M. E.; Giltrap, Andrew M.; Nagalingam, Gayathri; Britton, Warwick J.; Payne, Richard J. published an article.Computed Properties of 98946-18-0 The title of the article was Total synthesis of Ecumicin. And the article contained the following:

The first total synthesis of the potent anti-mycobacterial cyclic depsipeptide natural product ecumicin is described. Synthesis was achieved via a solid-phase strategy, incorporating the synthetic non-proteinogenic amino acids N-methyl-4-methoxy-L-tryptophan and threo-β-hydroxy-L-phenylalanine into the growing linear peptide chain. The synthesis employed key on-resin esterification and dimethylation steps as well as a final macrolactamization between the unusual N-methyl-4-methoxy-L-tryptophan unit and a bulky N-methyl-L-valine residue. The synthetic natural product possessed potent antimycobacterial activity against the virulent H37Rv strain of Mycobacterium tuberculosis (MIC90 = 312 nM). The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Computed Properties of 98946-18-0

The Article related to natural product cyclic depsipeptide antimycobacterial agent tuberculostatic drug, solid phase peptide synthesis esterification dimethylation macrolactamization steric effect and other aspects.Computed Properties of 98946-18-0

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

On August 3, 2021, Joshi, Bhaskar D.; Chisholm, John D. published an article.SDS of cas: 98946-18-0 The title of the article was Formation of pyrroloindolines via the alkylation of tryptamines with trichloroacetimidates. And the article contained the following:

Pyrroloindolines and related systems are present in a large number of complex natural products. These core structures have generated considerable synthetic interest, as many of the compounds possess challenging, elaborate structures and interesting biol. properties. Recently, we have focused on using trichloroacetimidates for the synthesis of these fascinating mols., e.g., I. Trichloroacetimidates can be used as an electrophilic source of an alkyl group to form the pyrroloindoline directly from tryptamine derivatives In this manner trichloroacetimidates provide a flexible solution to forming highly functionalized pyrroloindoline core structures, needing only a catalytic amount of a Lewis acid to effect the requisite transformations. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).SDS of cas: 98946-18-0

The Article related to pyrroloindoline preparation electrophilic alkylation cyclization tryptamine trichloroacetimidate, alkylation, heterocycle, pyrroloindoline, trichloroacetimidate, tryptamine and other aspects.SDS of cas: 98946-18-0

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

On July 21, 2021, Nair, Roshna V.; Farrukh, Aleeza; del Campo, Aranzazu published an article.Application of 98946-18-0 The title of the article was Light-Regulated Angiogenesis via a Phototriggerable VEGF Peptidomimetic. And the article contained the following:

The application of growth factor based therapies in regenerative medicine is limited by the high cost, fast degradation kinetics, and the multiple functions of these mols. in the cell, which requires regulated delivery to minimize side effects. Here a photoactivatable peptidomimetic of the vascular endothelial growth factor (VEGF) that allows the light-controlled presentation of angiogenic signals to endothelial cells embedded in hydrogel matrixes is presented. A photoresponsive analog of the 15-mer peptidomimetic Ac-KLTWQELYQLKYKGI-NH2 (abbreviated PQK) is prepared by introducing a 3-(4,5-dimethoxy-2-nitrophenyl)-2-Bu (DMNPB) photoremovable protecting group at the Trp4 residue. This modification inhibits the angiogenic potential of the peptide temporally. Light exposure of PQK modified hydrogels provide instructive cues to embedded endothelial cells and promote angiogenesis at the illuminated sites of the 3D culture, with the possibility of spatial control. PQK modified photoresponsive biomaterials offer an attractive approach for the dosed delivery and spatial control of pro-angiogenic factors to support regulated vascular growth by just using light as an external trigger. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application of 98946-18-0

The Article related to vegf peptidomimetic phototriggerable light angiogenesis, light regulated angiogenesis, photoactivatable qk, photoactivatable peptides, photocaged tryptophan, photoresponsive hydrogels and other aspects.Application of 98946-18-0

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

On July 13, 2017, Ghosh, Sukhen C.; Hernandez Vargas, Servando; Rodriguez, Melissa; Kossatz, Susanne; Voss, Julie; Carmon, Kendra S.; Reiner, Thomas; Schonbrunn, Agnes; Azhdarinia, Ali published an article.Category: chlorides-buliding-blocks The title of the article was Synthesis of a Fluorescently Labeled 68Ga-DOTA-TOC Analog for Somatostatin Receptor Targeting. And the article contained the following:

Fluorescently labeled imaging agents can identify surgical margins in real-time to help achieve complete resections and minimize the likelihood of local recurrence. However, photon attenuation limits fluorescence-based imaging to superficial lesions or lesions that are a few millimeters beneath the tissue surface. Contrast agents that are dual-labeled with a radionuclide and fluorescent dye can overcome this limitation and combine quant., whole-body nuclear imaging with intraoperative fluorescence imaging. Using a multimodality chelation (MMC) scaffold, IRDye 800CW was conjugated to the clin. used somatostatin analog, 68Ga-DOTA-TOC, to produce the dual-labeled analog, 68Ga-MMC(IRDye 800CW)-TOC, with high yield and specific activity. In vitro pharmacol. assays demonstrated retention of receptor-targeting properties for the dual-labeled compound with robust internalization that was somatostatin receptor (SSTR) 2-mediated. Biodistribution studies in mice identified the kidneys as the primary excretion route for 68Ga-MMC(IRDye 800CW)-TOC, along with clearance via the reticuloendothelial system. Higher uptake was observed in most tissues compared to 68Ga-DOTA-TOC but decreased as a function of time. The combination of excellent specificity for SSTR2-expressing cells and suitable biodistribution indicate potential application of 68Ga-MMC(IRDye 800CW)-TOC for intraoperative detection of SSTR2-expressing tumors. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Category: chlorides-buliding-blocks

The Article related to gallium 68 dota toc preparation somatostatin receptor fluorescent imaging, cancer fluorescent imaging somatostatin receptor gallium 68, dual labeling, nirf, pet, somatostatin receptor and other aspects.Category: chlorides-buliding-blocks

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

On September 30, 2017, Castillo-Pazos, Durbis J.; MacMillan, Derek published an article.Computed Properties of 98946-18-0 The title of the article was Investigation of cysteine as an activator of side-chain N→S acyl transfer and tail-to-side-chain cyclization. And the article contained the following:

N→S Acyl transfer is a popular method for the post-synthesis production of peptide Cα-thioesters for use in native chem. ligation and for the synthesis of head-to-tail cyclic peptides. Meanwhile thioester formation at the side chain of aspartic or glutamic acids, leading to tail-to-side-chain-cyclized species, is less common. Herein we explore the potential for cysteine to function as a latent thioester when appended to the side chain of glutamic acid. Initial insights gained through study of C-terminal β-alanine as a model for the increased chain length were ultimately applied to peptide macrocyclization. Our results emphasize the increased barrier to acyl transfer at the glutamic acid side chain and indicate how a slow reaction, facilitated by cysteine itself, may be accelerated by fine-tuning of the stereoelectronic environment. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Computed Properties of 98946-18-0

The Article related to cyclic peptide synthesis cysteine activator thioester macrocyclization kinetics, solid phase peptide synthesis acyl transfer macrocyclization ncl, agardhipeptin a analog cyclization and other aspects.Computed Properties of 98946-18-0

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

Huang, Yong; Zhang, Lu; Wang, Meng; Li, Chengze; Zheng, Wei; Chen, Hualong; Liang, Ying; Wu, Zehui published an article in 2022, the title of the article was Optimization of Precursor Synthesis Conditions of (2S,4S)4-[18F]FPArg and Its Application in Glioma Imaging.Application In Synthesis of tert-Butyl trichloroacetimidate And the article contains the following content:

Although the tracer (2S,4S)4-[18F]FPArg is expected to provide a powerful imaging method for the diagnosis and treatment of clin. tumors, it has not been realized due to the low yield of chem. synthesis and radiolabeling. A simple synthetic method for the radiolabeled precursor of (2S,4S)4-[18F]FPArg in stable yield was obtained by adjusting the sequence of the synthetic steps. Furthermore, the biodistribution experiments confirmed that (2S,4S)4-[18F]FPArg could be cleared out quickly in wild type mouse. Cell uptake experiments and U87MG tumor mouse microPET-CT imaging experiments showed that the tumor had high uptake of (2S,4S)4-[18F]FPArg and the clearance was slow, but (2S,4S)4-[18F]FPArg was rapidly cleared in normal brain tissue. MicroPET-CT imaging of nude mice bearing orthotopic HS683-Luc showed that (2S,4S)4-[18F]FPArg can penetrate blood-brain barrier and image gliomas with a high contrast. Therefore, (2S,4S)4-[18F]FPArg is expected to be further applied in the diagnosis and efficacy evaluation of clin. glioma. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application In Synthesis of tert-Butyl trichloroacetimidate

The Article related to carbamimidoyl carboxyaminomethyl carboxyamino fluoroheptanoic acid glioma imaging optimization, (2s,4s)4–[18f]fparg, amino acid, glioma imaging, positron emission tomography, tracer and other aspects.Application In Synthesis of tert-Butyl trichloroacetimidate

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

On December 7, 2020, Zhao, Ruiyue; Ploessl, Karl; Zha, Zhihao; Choi, Seokrye; Alexoff, David; Zhu, Lin; Kung, Hank F. published an article.Category: chlorides-buliding-blocks The title of the article was Synthesis and Evaluation of 68Ga- and 177Lu-Labeled (R)- vs (S)-DOTAGA Prostate-Specific Membrane Antigen-Targeting Derivatives. And the article contained the following:

Prostate-specific membrane antigen (PSMA) is overexpressed in prostate cancer cells and therefore is an attractive target for prostate cancer diagnosis and radionuclide therapy. Recently, published results from clin. studies using a new PSMA-targeting PET imaging agent, [68Ga]Ga-PSMA-093 ([68Ga]Ga-HBED-CC-O-carboxymethyl-Tyr-CO-NH-Glu), support the development of this agent for the diagnosis of prostate cancer. In this study, the HBED-CC chelating group in PSMA-093 was replaced by stereoselective (R)- or (S)-DOTAGA. This chelating group serves not only for chelating 68Ga but is also amendable for complexing other radioactive metals for radionuclide therapy. The corresponding optically pure (R)- and (S)-[68Ga/177Lu]-DOTAGA derivatives, (R)-[68Ga/177Lu]-13 and (S)-[68Ga/177Lu]-13, were successfully prepared Comparison of radiolabeling, binding affinity, cell uptake, and biodistribution between the two isomers was performed. Radiolabeling of (R)-[177Lu]Lu-13 and (S)-[177Lu]Lu-13 at 50°C suggested that rates of complex formation were time-dependent and the formation of (S)-[177Lu]Lu-13 was distinctly faster. The rates of complex formation for the corresponding 68Ga agents were comparable between structural isomers. The natGa and natLu equivalent showed high binding PSMA affinity (IC50 = 24-111 nM), comparable to that of the parent agent, [natGa]Ga-PSMA-093 (IC50 = 34.0 nM). Results of cell uptake and biodistribution studies in PSMA-expressing PC3-PIP tumor-bearing mice appeared to show no difference between the labeled (R)- and (S)-isomers. This is the first time that a pair of [68Ga/177Lu]-(R)- and (S)-DOTAGA isomers of PSMA agents were evaluated. Results of biol. studies between the isomers showed no noticeable difference; however, the distinctions on the rate of Lu complex formation should be considered in the development of new 177Lu-DOTAGA-based radionuclide therapy agents in the future. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Category: chlorides-buliding-blocks

The Article related to gallium lutetium dotag chelating agent optical isomer radionuclide therapy, dotaga, psma, biodistribution, cell uptake, chelating agents, gallium, lutetium, optical isomers, prostate cancer and other aspects.Category: chlorides-buliding-blocks

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

On August 1, 2017, Koshizawa, Tomoaki; Morimoto, Toshiharu; Watanabe, Gen; Watanabe, Toshiaki; Yamasaki, Nao; Sawada, Yoshikazu; Fukuda, Tomoaki; Okuda, Ayumu; Shibuya, Kimiyuki; Ohgiya, Tadaaki published an article.Application of 98946-18-0 The title of the article was Optimization of a novel series of potent and orally bioavailable GPR119 agonists. And the article contained the following:

We describe the discovery and optimization of a novel series of furo[3,2-d]pyrimidines as G protein-coupled receptor 119 agonists. Agonistic activity of 4 (EC50 = 129 nM) was improved by replacing the intramol. hydrogen bond between the fluorine atom and the aniline hydrogen in the head moiety with a covalent C-C bond to enhance conformational restriction, which consequently gave a lead compound 12 (EC50 = 53 nM). Optimized compound 26, which was identified by the further optimization of 12, exhibited potent activity (EC50 = 42 nM) with improved clearance in liver microsomes and induced a 33% reduction in blood glucose area under the curve at a dose of 10 mg/kg in an oral glucose tolerance test in C57BL/6N mice. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application of 98946-18-0

The Article related to furo pyrimidine derivative preparation oral gpr119 agonist diabetes, furo[3,2-d]pyrimidine, gpr119 agonists, intramolecular hydrogen bond, restricted conformation, type 2 diabetes mellitus and other aspects.Application of 98946-18-0

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