Category: 98946-18-0

Cui, Ji-Bin; Wei, Xiao-Xiong; Zhao, Rui; Zhu, Huixia; Shi, Jing; Bierer, Donald; Li, Yi-Ming published an article in 2021, the title of the article was Chemical synthesis of disulfide surrogate peptides by using beta-carbon dimethyl modified diaminodiacids.Name: tert-Butyl trichloroacetimidate And the article contains the following content:

The replacement of disulfide bridges with metabolically stable isosteres is a promising strategy to improve the stability of disulfide-rich polypeptides towards reducing agents and isomerases. A diaminodiacid-based strategy is one of the most effective methods to construct disulfide bond mimics, but modified diaminodiacids have not been developed till now. Inspired by the fact that alkylation of disulfide bonds can regulate the activity of polypeptides, herein, we report the first example of thioether bridged diaminodiacids incorporating Cys Cβ di-Me modification, obtained by penicillamine (Pen)-based thiol alkylation. The utility of these new diaminodiacids was demonstrated by the synthesis of disulfide surrogates of oxytocin containing a short-span disulfide bond and of KIIIA with large-span disulfide bonds. This new type of synthetic bridge further extends the diaminodiacid toolbox to facilitate the study of the structure-activity relationship of disulfide-rich peptides. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Name: tert-Butyl trichloroacetimidate

The Article related to peptide disulfide surrogate synthesis betacarbon dimethyl diaminodiacid, penicillamine thiol disulfide bond alkylation steric hindrance, oxytocin disulfide surrogates synthesis conotoxin kiiia analog, solid phase peptide synthesis oxidative cyclization ncl folding and other aspects.Name: tert-Butyl trichloroacetimidate

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

On June 5, 2020, Shabani, Sadegh; Hutton, Craig A. published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Total synthesis of Seongsanamide B. And the article contained the following:

The first total synthesis of the bicyclic depsipeptide natural product seongsanamide B is described. The successful approach employed solid-phase peptide synthesis of a core heptapeptide, incorporating on-resin esterification, followed by solution-phase macrolactamization and a late stage intramol. Evans-Chan-Lam coupling to generate the biaryl ether of the isodityrosine unit. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to bicyclic depsipeptide natural product seongsanamide b total synthesis, seongsanamide natural product antiallergic agent drug, solid phase synthesis peptide coupling heptapeptide esterification macrolactamization, evans chan lam coupling isodityrosine biaryl ether and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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

On September 4, 2020, He, Tingting; Peng, Lei; Li, Shan; Hu, Fangli; Xie, Chuandong; Huang, Shengli; Jia, Shiqi; Qin, Wenling; Yan, Hailong published an article.Product Details of 98946-18-0 The title of the article was Chiral Naphthyl-C2-Indole as Scaffold for Phosphine Organocatalysis: Application in Asymmetric Formal [4 + 2] Cycloaddition Reactions. And the article contained the following:

The applications of a newly designed chiral naphthyl-C2-indole bifunctional phosphine organocatalyst I in stereoselective formal [4 + 2] cycloaddition reactions were reported. The chiral naphthyl-C2-indole skeleton was introduced to bifunctional phosphine organocatalysis for the first time, and excellent stereocontrol was achieved in formal [4 + 2] cycloaddition reactions of dicyanomethyleneoxindoles II (R1 = Me, MeOCH2, H2C:CHCH2, PhCH2, Ph; R2 = H, 5-Me, 7-Me, 6-MeO, 6-MeO, 7-F3C, 5-Cl, 5-Br, 6-Br) with pentadienones (E)-R3CH:CHCOCH:CH2 (R3 = Ph, 4-MeC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 2-furyl) and of oxoindolylideneacetates III (R4 = H, Me, MeOCH2, H2C:CHCH2, Boc, Ph, PhCH2, PhCO; R5 = H, 5-Me, 7-Me, 5, 7-Me2, 5-MeO, 6-MeO, 5-F, 5-Cl, 6-Cl, 5-Br, 6-Br, 7-Br; X = CH, N) with 3-acryloylbenzofuran. With the optimal catalyst, chiral spirooxindoles IV (R1 = Me, MeOCH2, H2C:CHCH2, PhCH2, Ph; R2 = H, 5-Me, 7-Me, 6-MeO, 6-MeO, 7-F3C, 5-Cl, 5-Br, 6-Br; R3 = Ph, 4-MeC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 2-furyl) and spirodibenzofuranoxindoles V (R4 = H, Me, MeOCH2, H2C:CHCH2, Boc, Ph, PhCH2, PhCO; R5 = H, 5-Me, 7-Me, 5, 7-Me2, 5-MeO, 6-MeO, 5-F, 5-Cl, 6-Cl, 5-Br, 6-Br, 7-Br; X = CH, N) were produced in moderate to good yields with excellent stereoselectivities (up to >99% ee, >20:1 dr). The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0

The Article related to phosphinoindolylnaphthol nonracemic preparation organocatalyst, spirooxindole spirodibenzofuranoxindole diastereoselective enantioselective preparation, stereoselective formal cycloaddition dicyanomethyleneoxindole pentadienone phosphinoindolylnaphthol catalyst and other aspects.Product Details of 98946-18-0

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

On May 1, 2017, Xu, Jiayi; Lin, Songnian; Myers, Robert W.; Trujillo, Maria E.; Pachanski, Michele J.; Malkani, Sunita; Chen, Hsuan-shen; Chen, Zhesheng; Campbell, Brian; Eiermann, George J.; Elowe, Nadine; Farrer, Brian T.; Feng, Wen; Fu, Qinghong; Kats-Kagan, Roman; Kavana, Michael; McMasters, Daniel R.; Mitra, Kaushik; Tong, Xinchun; Xu, Libo; Zhang, Fengqi; Zhang, Rui; Addona, George H.; Berger, Joel P.; Zhang, Bei; Parmee, Emma R. published an article.Recommanded Product: 98946-18-0 The title of the article was Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. And the article contained the following:

Systemically acting glucokinase activators (GKA) have been demonstrated in clin. trials to effectively lower blood glucose in patients with type II diabetes. However, mechanism-based hypoglycemia is a major adverse effect that limits the therapeutic potential of these agents. The authors hypothesized that the predominant mechanism leading to hypoglycemia is GKA-induced excessive insulin secretion from pancreatic β-cells at (sub-)euglycemic levels. The authors further hypothesized that restricting GK activation to hepatocytes would maintain glucose-lowering efficacy while significantly reducing hypoglycemic risk. Here the authors report the discovery of a novel series of carboxylic acid substituted GKAs based on pyridine-2-carboxamide. These GKAs exhibit preferential distribution to the liver vs. the pancreas in mice. SAR studies led to the identification of a potent and orally active hepatoselective GKA, compound I. GKA I demonstrated robust glucose lowering efficacy in high fat diet-fed mice at doses ≥10 mpk, with ≥70-fold liver:pancreas distribution, minimal effects on plasma insulin levels, and significantly reduced risk of hypoglycemia. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: 98946-18-0

The Article related to glucokinase activator antidiabetic diabetes, diabetes, glucokinase, glucokinase activator (gka), glucose homeostasis, glucose metabolism, hepatoselective, hepatospecific, hexokinase iv, liver preferring, pyridine-2-carboxamide, type ii diabetes mellitus and other aspects.Recommanded Product: 98946-18-0

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

On June 9, 2016, Chiotellis, Aristeidis; Muller Herde, Adrienne; Rossler, Simon L.; Brekalo, Ante; Gedeonova, Erika; Mu, Linjing; Keller, Claudia; Schibli, Roger; Kramer, Stefanie D.; Ametamey, Simon M. published an article.Category: chlorides-buliding-blocks The title of the article was Synthesis, radiolabeling, and biological evaluation of 5-Hydroxy-2-[18F]fluoroalkyl-tryptophan analogues as potential PET radiotracers for tumor imaging. And the article contained the following:

Aiming at developing mechanism-based amino acid 18F-PET tracers for tumor imaging, we synthesized two 18F-labeled analogs of 5-hydroxy-L-[β-11C]tryptophan ([11C]5HTP) whose excellent in vivo performance in neuroendocrine tumors is mainly attributed to its decarboxylation by aromatic amino acid decarboxylase (AADC), an enzyme overexpressed in these malignancies. Reference compounds and precursors were synthesized following multistep synthetic approaches. Radiosynthesis of tracers was accomplished in good radiochem. yields (15-39%), high specific activities (45-95 GBq/μmol), and excellent radiochem. purities. In vitro cell uptake was sodium-independent and was inhibited ≥95% by 2-amino-2-norbornanecarboxylic acid (BCH) and ∼30% by arginine. PET imaging in mice revealed distinctly high tumor/background ratios for both tracers, outperforming the well-established O-(2-[18F]fluoroethyl)tyrosine ([18F]FET) tracer in a head-to-head comparison. Biol. evaluation revealed that the in vivo performance is most probably independent of any interaction with AADC. Nevertheless, the excellent tumor visualization qualifies the new tracers as interesting probes for tumor imaging worthy for further investigation. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Category: chlorides-buliding-blocks

The Article related to tryptophane hydroxy fluoro alkyl 18f synthesis radiolabeling tumor imaging, hydroxy tryptophane allylation danishevsky reaction protection hydroboration oxidation fluorination, phthaloyl hydroxytrypthophane benzylation krapcho decarboxylation reduction and other aspects.Category: chlorides-buliding-blocks

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

Cui, Ji-Bin; Wei, Xiao-Xiong; Zhao, Rui; Zhu, Huixia; Shi, Jing; Bierer, Donald; Li, Yi-Ming published an article in 2021, the title of the article was Chemical synthesis of disulfide surrogate peptides by using beta-carbon dimethyl modified diaminodiacids.Name: tert-Butyl trichloroacetimidate And the article contains the following content:

The replacement of disulfide bridges with metabolically stable isosteres is a promising strategy to improve the stability of disulfide-rich polypeptides towards reducing agents and isomerases. A diaminodiacid-based strategy is one of the most effective methods to construct disulfide bond mimics, but modified diaminodiacids have not been developed till now. Inspired by the fact that alkylation of disulfide bonds can regulate the activity of polypeptides, herein, we report the first example of thioether bridged diaminodiacids incorporating Cys Cβ di-Me modification, obtained by penicillamine (Pen)-based thiol alkylation. The utility of these new diaminodiacids was demonstrated by the synthesis of disulfide surrogates of oxytocin containing a short-span disulfide bond and of KIIIA with large-span disulfide bonds. This new type of synthetic bridge further extends the diaminodiacid toolbox to facilitate the study of the structure-activity relationship of disulfide-rich peptides. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Name: tert-Butyl trichloroacetimidate

The Article related to peptide disulfide surrogate synthesis betacarbon dimethyl diaminodiacid, penicillamine thiol disulfide bond alkylation steric hindrance, oxytocin disulfide surrogates synthesis conotoxin kiiia analog, solid phase peptide synthesis oxidative cyclization ncl folding and other aspects.Name: tert-Butyl trichloroacetimidate

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

On June 5, 2020, Shabani, Sadegh; Hutton, Craig A. published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Total synthesis of Seongsanamide B. And the article contained the following:

The first total synthesis of the bicyclic depsipeptide natural product seongsanamide B is described. The successful approach employed solid-phase peptide synthesis of a core heptapeptide, incorporating on-resin esterification, followed by solution-phase macrolactamization and a late stage intramol. Evans-Chan-Lam coupling to generate the biaryl ether of the isodityrosine unit. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to bicyclic depsipeptide natural product seongsanamide b total synthesis, seongsanamide natural product antiallergic agent drug, solid phase synthesis peptide coupling heptapeptide esterification macrolactamization, evans chan lam coupling isodityrosine biaryl ether and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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

On September 4, 2020, He, Tingting; Peng, Lei; Li, Shan; Hu, Fangli; Xie, Chuandong; Huang, Shengli; Jia, Shiqi; Qin, Wenling; Yan, Hailong published an article.Product Details of 98946-18-0 The title of the article was Chiral Naphthyl-C2-Indole as Scaffold for Phosphine Organocatalysis: Application in Asymmetric Formal [4 + 2] Cycloaddition Reactions. And the article contained the following:

The applications of a newly designed chiral naphthyl-C2-indole bifunctional phosphine organocatalyst I in stereoselective formal [4 + 2] cycloaddition reactions were reported. The chiral naphthyl-C2-indole skeleton was introduced to bifunctional phosphine organocatalysis for the first time, and excellent stereocontrol was achieved in formal [4 + 2] cycloaddition reactions of dicyanomethyleneoxindoles II (R1 = Me, MeOCH2, H2C:CHCH2, PhCH2, Ph; R2 = H, 5-Me, 7-Me, 6-MeO, 6-MeO, 7-F3C, 5-Cl, 5-Br, 6-Br) with pentadienones (E)-R3CH:CHCOCH:CH2 (R3 = Ph, 4-MeC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 2-furyl) and of oxoindolylideneacetates III (R4 = H, Me, MeOCH2, H2C:CHCH2, Boc, Ph, PhCH2, PhCO; R5 = H, 5-Me, 7-Me, 5, 7-Me2, 5-MeO, 6-MeO, 5-F, 5-Cl, 6-Cl, 5-Br, 6-Br, 7-Br; X = CH, N) with 3-acryloylbenzofuran. With the optimal catalyst, chiral spirooxindoles IV (R1 = Me, MeOCH2, H2C:CHCH2, PhCH2, Ph; R2 = H, 5-Me, 7-Me, 6-MeO, 6-MeO, 7-F3C, 5-Cl, 5-Br, 6-Br; R3 = Ph, 4-MeC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 2-furyl) and spirodibenzofuranoxindoles V (R4 = H, Me, MeOCH2, H2C:CHCH2, Boc, Ph, PhCH2, PhCO; R5 = H, 5-Me, 7-Me, 5, 7-Me2, 5-MeO, 6-MeO, 5-F, 5-Cl, 6-Cl, 5-Br, 6-Br, 7-Br; X = CH, N) were produced in moderate to good yields with excellent stereoselectivities (up to >99% ee, >20:1 dr). The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0

The Article related to phosphinoindolylnaphthol nonracemic preparation organocatalyst, spirooxindole spirodibenzofuranoxindole diastereoselective enantioselective preparation, stereoselective formal cycloaddition dicyanomethyleneoxindole pentadienone phosphinoindolylnaphthol catalyst and other aspects.Product Details 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.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 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