Category: 98946-18-0

On September 16, 2020, Moore, Maxwell J.; Qu, Shiwei; Tan, Ceheng; Cai, Yu; Mogi, Yuzo; Jamin Keith, D.; Boger, Dale L. published an article.Electric Literature of 98946-18-0 The title of the article was Next-Generation Total Synthesis of Vancomycin. And the article contained the following:

A next-generation total synthesis of vancomycin aglycon is detailed that was achieved in 17 steps (longest linear sequence, LLS) from the constituent amino acid subunits with kinetically controlled diastereoselective introduction of all three elements of atropisomerism. In addition to new syntheses of three of the seven amino acid subunits, highlights of the approach include a ligand-controlled atroposelective one-pot Miyaura borylation-Suzuki coupling sequence for introduction of the AB biaryl axis of chirality (>20:1 dr), an essentially instantaneous and scalable macrolactamization of the AB ring system nearly free of competitive epimerization (>30:1 dr), and two room-temperature atroposelective intramol. SNAr cyclizations for sequential CD (8:1 dr) and DE ring closures (14:1 dr) that benefit from both preorganization by the preformed AB ring system and subtle substituent effects. Combined with a protecting group free two-step enzymic glycosylation of vancomycin aglycon, this provides a 19-step total synthesis of vancomycin. The approach paves the way for large-scale synthetic preparation of pocket-modified vancomycin analogs that directly address the underlying mechanism of resistance to vancomycin. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Electric Literature of 98946-18-0

The Article related to vancomycin aglycon streamlined synthesis atropisomer diastereoselectivity macrocyclic ring, Carbohydrates: Amines and other aspects.Electric Literature of 98946-18-0

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

On December 27, 2019, Liu, Si-Xian; Tsai, Yun-Tzu; Lin, Yu-Tung; Li, Jia-Yue; Chang, Che-Chien published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Design and synthesis of trivalent Tn glycoconjugate polymers by nitroxide-mediated polymerization. And the article contained the following:

A new synthetic method for preparing Tn glycoconjugate polymers, containing tumor-associated carbohydrate antigens, by controlled living radical polymerization is reported. To mimic the authentic structures of Tn glycopeptide antigens and to explore the controlled living radical polymerization, three tumor-associated carbohydrate antigens (GalNAc, GalNAcα1-O-Ser, and GalNAcα1-O-Thr) were attached to a styrene-type monomer through a diethylene glycol spacer. Under nitroxide-mediated polymerization, controlled living radical polymerization proceeded to afford defined glycopeptide polymers with different Tn densities and compositions The polydispersity index (PDI) and mol. weights were increased and conversions were decreased upon increasing the concentration of Tn glycoconjugate monomers. The resulting Tn glycoconjugate polymers were characterized by NMR and IR. The spectral data indicate that the Tn glycoconjugate moiety did attach to the polymer chain and Tn glycoconjugate d. could be adjusted through the nitroxide-mediated polymerization conditions. The number of Tn units containing in the polymer chains could be estimated by NMR integration. This synthetic approach provides a new and efficient tool for constructing novel Tn glycoconjugate polymers. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to synthesis trivalent tn glycoconjugate polymer nitroxide mediated polymerization, Biochemical Methods: Synthesis and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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

On April 14, 2016, Bouhlel, Ahlem; Alyami, Wadha; Li, Aixiao; Yuan, Liya; Rich, Keith; McConathy, Jonathan published an article.Product Details of 98946-18-0 The title of the article was Effect of α-Methyl versus α-Hydrogen Substitution on Brain Availability and Tumor Imaging Properties of Heptanoic [F-18]Fluoroalkyl Amino Acids for Positron Emission Tomography (PET). And the article contained the following:

Two [18F]fluoroalkyl substituted amino acids differing only by the presence or absence of a Me group on the α-carbon, (S)-2-amino-7-[18F]fluoro-2-methylheptanoic acid ((S)-[18F]FAMHep, (S)-[18F]14) and (S)-2-amino-7-[18F]fluoroheptanoic acid ((S)-[18F]FAHep, (S)-[18F]15), were developed for brain tumor imaging and compared to the well-established system L amino acid tracer, O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET), in the delayed brain tumor (DBT) mouse model of high-grade glioma. Cell uptake, biodistribution, and PET/CT imaging studies showed differences in amino acid transport of these tracer by DBT cells. Recognition of (S)-[18F]15 but not (S)-[18F]14 by system L amino acid transporters led to approx. 8-10-fold higher uptake of the α-hydrogen substituted analog (S)-[18F]15 in normal brain. (S)-[18F]15 had imaging properties similar to those of (S)-[18F]FET in the DBT tumor model while (S)-[18F]14 afforded higher tumor to brain ratios due to much lower uptake by normal brain. These results have important implications for the future development of α-alkyl and α,α-dialkyl substituted amino acids for brain tumor imaging. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0

The Article related to fluolroalkyl amino acid preparation pet imaging agent brain tumor, Pharmaceuticals: Pharmaceutics and other aspects.Product Details of 98946-18-0

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

Budke, Brian; Tueckmantel, Werner; Miles, Kelsey; Kozikowski, Alan P.; Connell, Philip P. published an article in 2019, the title of the article was Optimization of drug candidates that inhibit the D-loop activity of RAD51.Safety of tert-Butyl trichloroacetimidate And the article contains the following content:

RAD51 is the central protein in homologous recombination (HR) repair, where it first binds ssDNA and then catalyzes strand invasion via a D-loop intermediate. Addnl., RAD51 plays a role in faithful DNA replication by protecting stalled replication forks; this requires RAD51 to bind DNA but may not require the strand invasion activity of RAD51. We previously described a small-mol. inhibitor of RAD51 named RI(dl)-2 (RAD51 inhibitor of D-loop formation #2, hereafter called 2h(I)), which inhibits D-loop activity while sparing ssDNA binding. However, I is limited in its ability to inhibit HR in vivo, preventing only about 50 % of total HR events in cells. We sought to improve upon this by performing a structure-activity relationship (SAR) campaign for more potent analogs of I. Most compounds were prepared from 1-(2-aminophenyl)pyrroles by forming the quinoxaline moiety either by condensation with aldehydes, then dehydrogenation of the resulting 4,5-dihydro intermediates, or by condensation with N,N’-carbonyldiimidazole, chlorination, and installation of the 4-substituent through Suzuki-Miyaura coupling. Many analogs exhibited enhanced activity against human RAD51, but in several of these compounds the increased inhibition was due to the introduction of dsDNA intercalation activity. We developed a sensitive assay to measure dsDNA intercalation, and identified two analogs of I that promote complete HR inhibition in cells while exerting minimal intercalation activity. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Safety of tert-Butyl trichloroacetimidate

The Article related to rad51 d loop homologous recombination quinoxaline, dna repair, biological activity, cancer, inhibitors, structure-activity relationships, Pharmacology: Structure-Activity and other aspects.Safety of tert-Butyl trichloroacetimidate

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

On March 14, 2019, Krall, Jacob; Bavo, Francesco; Falk-Petersen, Christina B.; Jensen, Claus H.; Nielsen, Julie O.; Tian, Yongsong; Anglani, Valeria; Kongstad, Kenneth T.; Piilgaard, Louise; Nielsen, Birgitte; Gloriam, David E.; Kehler, Jan; Jensen, Anders A.; Harpsoee, Kasper; Wellendorph, Petrine; Froelund, Bente published an article.Name: tert-Butyl trichloroacetimidate The title of the article was Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic acid as a new class of ligands selective for the γ-hydroxybutyric acid (GHB) high-affinity binding sites. And the article contained the following:

Gabazine, a γ-aminobutyric acid type A (GABAA) receptor antagonist, has previously been reported to inhibit the binding of [3H]NCS-382, a representative ligand of the high-affinity binding site for the neuroactive substance γ-hydroxybutyric acid (GHB). We herein report a study on the structural determinants of gabazine for binding to (i) the orthosteric binding site of the GABAA receptor and (ii) the high-affinity GHB binding site. Expanding the structural diversity of available ligands for the high-affinity GHB binding sites, this study identified 2-(imidazo[1,2-b]pyridazin-2-yl)acetic acid as a novel ligand-scaffold leading to analogs with relatively high affinity (Ki 0.19-2.19 μM) and >50 times selectivity for the [3H]NCS-382 over [3H]muscimol binding sites. These results highlight that gabazine interacts with the high-affinity GHB and orthosteric GABAA receptor binding sites differently and that distinct analogs can be generated to select between them. To facilitate further in vivo studies, a promising prodrug candidate for brain delivery was identified. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Name: tert-Butyl trichloroacetimidate

The Article related to gabazine gamma hydroxybutyric acid high affinity binding site gabaa, Pharmacology: Structure-Activity and other aspects.Name: tert-Butyl trichloroacetimidate

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

On November 22, 2017, Rai, Ganesha; Brimacombe, Kyle R.; Mott, Bryan T.; Urban, Daniel J.; Hu, Xin; Yang, Shyh-Ming; Lee, Tobie D.; Cheff, Dorian M.; Kouznetsova, Jennifer; Benavides, Gloria A.; Pohida, Katie; Kuenstner, Eric J.; Luci, Diane K.; Lukacs, Christine M.; Davies, Douglas R.; Dranow, David M.; Zhu, Hu; Sulikowski, Gary; Moore, William J.; Stott, Gordon M.; Flint, Andrew J.; Hall, Matthew D.; Darley-Usmar, Victor M.; Neckers, Leonard M.; Dang, Chi V.; Waterson, Alex G.; Simeonov, Anton; Jadhav, Ajit; Maloney, David J. published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). And the article contained the following:

The authors report the discovery and medicinal chem. optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quant. high-throughput screening paradigm facilitated hit identification, while structure-based design and multiparameter optimization enabled the development of compounds with potent enzymic and cell-based inhibition of LDH enzymic activity. Lead compounds such as 63 exhibit low nM inhibition of both LDHA and LDHB, submicromolar inhibition of lactate production, and inhibition of glycolysis in MiaPaCa2 pancreatic cancer and A673 sarcoma cells. Moreover, robust target engagement of LDHA by lead compounds was demonstrated using the cellular thermal shift assay (CETSA), and drug-target residence time was determined via SPR. Anal. of these data suggests that drug-target residence time (off-rate) may be an important attribute to consider for obtaining potent cell-based inhibition of this cancer metabolism target. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to pyrazole preparation lactate dehydrogenase inhibitor, Pharmacology: Structure-Activity and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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

On January 1, 2021, Ohsawa, Kosuke; Ochiai, Shota; Kubota, Junya; Doi, Takayuki published an article.Electric Literature of 98946-18-0 The title of the article was Gold-catalyzed amide/carbamate-linked N,O-acetal formation with bulky amides and alcohols. And the article contained the following:

A gold-catalyzed N,O-acetal formation was established to construct an amide/carbamate-linked N,O-acetal substructure with bulky alcs. The acyliminium cation species generated from o-alkynylbenzoic acid ester in the presence of a gold catalyst is highly reactive and underwent nucleophilic attack of various bulky alcs. and phenols at room temperature under neutral conditions, leading to the corresponding N,O-acetals in yields of 34-89% with good functional group tolerance. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Electric Literature of 98946-18-0

The Article related to amide carbamate linked nitrogen oxygen acetal preparation, cyclopropylmethylaminomethyl alkynylbenzoate nucleophilic addition alc, Alicyclic Compounds: Cyclopropanes and other aspects.Electric Literature of 98946-18-0

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

Shimodaira, Shingo; Iwaoka, Michio published an article in 2019, the title of the article was Synthesis of selenocysteine-containing dipeptides modeling the active site of thioredoxin reductase.Synthetic Route of 98946-18-0 And the article contains the following content:

Four cyclic dipeptides modeling the active site of thioredoxin reductase (TrxR), UU, CU, UC, and CC, where U and C represent selenocystine and cystine, resp., were synthesized and their glutathione peroxidase (GPx)-like catalytic activity was evaluated by the reaction of hydrogen peroxide (H2O2) with glutathione (GSH) in the presence of glutathione reductase (GR). Among these, only UC exhibited the significant antioxidant capacity, suggesting that an at. environment around the Se-S bond is relevant to the reactivity toward a thiol substrate. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Synthetic Route of 98946-18-0

The Article related to thioredoxin reductase trxr active site mimic cyclic dipeptide selenocysteine, Enzymes: Structure-Conformation-Active Site and other aspects.Synthetic Route of 98946-18-0

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

Nakashima, Kazuma; Iikuni, Shimpei; Watanabe, Hiroyuki; Ono, Masahiro published an article in 2021, the title of the article was Development of a novel radiotheranostic platform with a DOTA-based trifunctional chelating agent.Computed Properties of 98946-18-0 And the article contains the following content:

Radiotheranostics has attracted attention as a powerful strategy for treating cancer patients with precision medicine. We designed and synthesized a novel DOTA-based trifunctional agent, ADIBO-DOTADG-ALB (ADA), which allowed compounds with targeting ligands, radiometals, and an albumin binder to be readily prepared ADA exhibited promising properties as a theranostic platform. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Computed Properties of 98946-18-0

The Article related to dota based trifunctional indium labeled chelation complex radiotheranostic, Placeholder for records without volume info and other aspects.Computed Properties of 98946-18-0

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

On February 25, 2022, Ochi, Akihiro; Yoritate, Makoto; Miyamoto, Tomofumi; Usui, Kazuteru; Yusakul, Gorawit; Putalun, Waraporn; Tanaka, Hiroyuki; Hirai, Go; Morimoto, Satoshi; Sakamoto, Seiichi published an article.Application In Synthesis of tert-Butyl trichloroacetimidate The title of the article was Harringtonine Ester Derivatives with Enhanced Antiproliferative Activities against HL-60 and HeLa Cells. And the article contained the following:

Harringtonine (HT), produced from Cephalotaxus species, is known to exhibit potent antiproliferative activity against myeloid leukemia cells by inhibiting protein synthesis. A previous study using acute promyelocytic leukemia (HL-60) cells raised the possibility that the C-5′ Me group of HT plays an important role in regulating leukemia cell line antiproliferative activity. In order to investigate the effect of hydrocarbon chains at C-5′ on the resultant activity, the C-5′ Me group was replaced with various straight- and branched-chain hydrocarbons using the corresponding alcs., and their antiproliferative activity against HL-60 and HeLa cells was investigated. As a result, 4′-n-heptyl-4′-demethylharringtonine (1f, n-heptyl derivative)(I) showed the most potent cytotoxicity among the HT ester derivatives produced, with IC50 values of 9.4 nM and 0.4 μM for HL-60 and HeLa cells, resp. Interestingly, the cytotoxicity of derivative 1f against HL-60 and HeLa cells resp. was ~5 (IC50 = 50.5 nM) and ~10 times (IC50 = 4.0 μM) those of HT and ~2 (IC50 = 21.8 nM) and ~4 times (IC50 = 1.7 μM) more than homoharringtonine (HHT). These results demonstrate the potential of the derivative 1f as a lead compound against leukemia. 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 harringtonine ester derivative antiproliferative leukemia cephalotaxus, Placeholder for records without volume info and other aspects.Application In Synthesis of tert-Butyl trichloroacetimidate

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