Tag: 200-300

On March 28, 2021, Andrade-Sampedro, Paula; Matxain, Jon M.; Correa, Arkaitz published an article.Category: chlorides-buliding-blocks The title of the article was Pd-Catalyzed C(sp2)-H Alkoxycarbonylation of Phenethyl- and Benzylamines with Chloroformates as CO Surrogates. And the article contained the following:

Herein, an unprecedented Pd-catalyzed C(sp2)-H alkoxycarbonylation of phenylalanine derivatives and other amines featuring picolinamide as the directing group (DG) to afford the corresponding alkoxycarbonylated products, e.g., I (R = H, CO2Et), is reported. This oxidative coupling is distinguished by its scalability, operational simplicity, and avoids the use of toxic carbon monoxide as the C1 source. Remarkably, the easy cleavage of the DG enabled the efficient assembly of isoindolinone compounds D. Functional Theory calculations support a PdII/PdIV catalytic cycle. 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 alkoxycarbonylated phenylalanine derivative site selective preparation, phenylalanine chloroformate alkoxycarbonylation palladium catalyst, c−h functionalization, dft calculations, alkoxycarbonylation, benzylamine, phenylalanine and other aspects.Category: chlorides-buliding-blocks

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

On May 14, 2020, Shepard, Stacey; Combs, Andrew P. published a patent.SDS of cas: 877149-10-5 The title of the patent was Preparation of heterocyclic derivatives as PI3K inhibitors. And the patent contained the following:

This invention relates to compounds I [Z = CZ1 or N; Z1 and R12 = (independently) H, D, OH, NO2, etc.; R1 = H, D, halo, alkyl, etc.; R2 = H, D, halo, alkyl, etc.; R6 = H, D, halo, alkyl, etc.; X9 = (un)substituted NH or CH2; X11 = (un)substituted NH or CH2; R = H, alkyl, alkenyl, etc.] or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases. E.g., a multi-step synthesis of (S)-II, starting from 4-bromopyridine-2-carbonitrile, was disclosed. The exemplified compounds I were tested in the PI3Kγ, PI3Kδ, and PI3Kγ THP1 RPS6 ELISA assays (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of Methyl 4-bromo-2-chloro-6-methylbenzoate(cas: 877149-10-5).SDS of cas: 877149-10-5

The Article related to heterocyclic derivative preparation pi3k gamma inhibitor antitumor cardiovascular, autoimmune neurodegenerative disease treatment heterocyclic derivative preparation pi3k gamma, heteroarylpyridazinyl heteroarylpyridyl isoindolinone indazole preparation pi3k gamma inhibitor and other aspects.SDS of cas: 877149-10-5

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

On March 23, 2022, Varkhedkar, Rajesh; Yang, Fan; Dontha, Rakesh; Zhang, Jianglin; Liu, Jiyong; Spingler, Bernhard; van der Veen, Stijn; Duttwyler, Simon published an article.HPLC of Formula: 14602-86-9 The title of the article was Natural-Product-Directed Catalytic Stereoselective Synthesis of Functionalized Fused Borane Cluster-Oxazoles for the Discovery of Bactericidal Agents. And the article contained the following:

The identification of an alternative chem. space to address the global challenge posed by emerging antimicrobial resistance is very much needed for the discovery of novel antimicrobial lead compounds B clusters are currently being explored in drug discovery due to their unique steric and electronic properties. However, the challenges associated with the synthesis and derivatization techniques of these compounds have limited their utility in the rapid construction of a library of mols. for screening against various biol. targets as an alternative mol. platform. Herein, the authors report a transition-metal-catalyzed regioselective direct B-H alkylation-annulation of the closo-dodecaborate anion with natural products such as menthol and camphor as the directing groups. This method allowed the rapid construction of a library of 1,2,3-trisubstituted clusters, which were evaluated in terms of their antibacterial activity against WHO priority pathogens. Several of the synthesized dodecaborate derivatives displayed medium- to high-level bactericidal activity against Gram-pos. and Gram-neg. bacteria. 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 mentholdiboraoxazole fused carborane preparation antibacterial activity, crystal structure mentholdiboraoxazole fused carborane, mol structure mentholdiboraoxazole fused carborane, rhodium catalyzed regioselective alkylation annulation dodecaborate anion styrene derivative and other aspects.HPLC of Formula: 14602-86-9

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

On June 3, 2016, Castanheiro, Thomas; Suffert, Jean; Gulea, Mihaela; Donnard, Morgan published an article.Application of 14602-86-9 The title of the article was Aerobic Copper-Mediated Domino Three-Component Approach to 2-Aminobenzothiazole Derivatives. And the article contained the following:

N-(2-Benzothiazolyl)amides were prepared by the three-component reactions of 2,2′-diaminodiaryl disulfides (or the hydrochloride of an aminotrifluoromethylbenzenethiol), copper cyanide, and acyl, dimethylthiocarbamoyl, or L-menthyloxyformyl chlorides, Boc anhydride, and Ph isocyanate using an oxidative copper-mediated S-cyanation as a key step followed by cyclization and acylation. The reaction proceeds by a mechanism involving an intermol. migration of the acyl group, as scrambling of acyl groups in reactions of acylaminophenyl disulfides was found. The structure of N-(2-benzothiazolyl)-2,5-difluorobenzamide was determined by X-ray crystallog. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Application of 14602-86-9

The Article related to benzothiazolyl amide chemoselective preparation, copper cyanide aminoaryl disulfide thiol acyl chloride chemoselective reaction, oxidative cyanation cyclization acylation reaction copper cyanide aminoaryl disulfide, fluorobenzamide benzothiazolyl mol crystal structure and other aspects.Application of 14602-86-9

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 May 6, 2016, Vincent, Adrien; Deschamps, Damien; Martzel, Thomas; Lohier, Jean-Francois; Richards, Christopher J.; Gaumont, Annie-Claude; Perrio, Stephane published an article.SDS of cas: 14602-86-9 The title of the article was Enantiomerically Pure [2.2]Paracyclophane-4-thiol: A Planar Chiral Sulfur-Based Building Block Readily Available by Resolution with an Amino Acid Chiral Auxiliary. And the article contained the following:

Acyl chloride of N-phthaloyl-(S)-isoleucine is an efficient chiral auxiliary for the resolution of (±)-[2.2]paracyclophane-4-thiol. A preparative protocol, based on the conversion into diastereoisomeric thiolesters and separation by two fractional crystallizations and column chromatog., was developed. Deprotection with LiAlH4 allowed isolation of the individual thiol enantiomers in good yield (∼40%) and high enantiomeric purity (ee >93%). The absolute configurations were determined by comparison of the optical rotation value of the products with literature data and were confirmed by X-ray crystallog. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).SDS of cas: 14602-86-9

The Article related to chiral paracyclophane thiol preparation resolution amino acid auxiliary, acyl chloride phthaloyl isoleucine auxiliary preparation paracyclophane resolution, crystal mol structure paracyclophane thiol, phthaloyl leucine auxiliary preparation crystal mol structure and other aspects.SDS of cas: 14602-86-9

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