Tag: 200-300

On November 28, 2020, Hawkins, Paige M. E.; Tran, Wendy; Nagalingam, Gayathri; Cheung, Chen-Yi; Giltrap, Andrew M.; Cook, Gregory M.; Britton, Warwick J.; Payne, Richard J. published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Total synthesis and antimycobacterial activity of Ohmyungsamycin A, Deoxyecumicin, and Ecumicin. And the article contained the following:

The ohmyungsamycin and ecumicin natural product families are structurally related cyclic depsipeptides that display potent antimycobacterial activity. Herein the total syntheses of ohmyungsamycin A, deoxyecumicin, and ecumicin are reported, together with the direct biol. comparison of members of these natural product families against Mycobacterium tuberculosis (Mtb), the etiol. agent of tuberculosis (TB). The synthesis of each of the natural products employed a solid-phase strategy to assemble the linear peptide precursor, involving a key on-resin esterification and an optional on-resin dimethylation step, before a final solution-phase macrolactamization between the non-proteinogenic N-methyl-4-methoxy-L-tryptophan amino acid and a bulky N-methyl-L-valine residue. The synthetic natural products possessed potent antimycobacterial activity against Mtb with MIC90’s ranging from 110-360 nM and retained activity against Mtb in Mtb-infected macrophages. Deoxyecumicin also exhibited rapid bactericidal killing against Mtb, sterilizing cultures after 21 days. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to natural product cyclic peptide ohmyungsamycin deoxyecumicin ecumicin total synthesis, cyclopeptide antimycobacterial agent tuberculostatic drug, deoxyecumicin sterilizing agent mycobacterium tuberculosis, solid phase peptide synthesis esterification dimethylation macrolactamization, natural products, peptides, solid-phase synthesis, total synthesis, tuberculosis and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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

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

On May 14, 2020, Shepard, Stacey; Ai, Yanran; Combs, Andrew P.; Shvartsbart, Artem published a patent.Recommanded Product: Methyl 4-bromo-2-chloro-6-methylbenzoate 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 [R1 = 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.TFA, starting from Me 4-bromo-2-(bromomethyl)benzoate and (S)-1-cyclopropylethan-1-amine, 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).Recommanded Product: Methyl 4-bromo-2-chloro-6-methylbenzoate

The Article related to heterocyclic derivative preparation pi3k gamma inhibitor antitumor cardiovascular, autoimmune neurodegenerative disease treament heterocyclic derivative preparation pi3k gamma, pyrazinyl isoindolinone indazole preparation pi3k gamma inhibitor, pyrazinamine oxoindolinyl indazolyl preparation pi3k gamma inhibitor antitumor cardiovascular and other aspects.Recommanded Product: Methyl 4-bromo-2-chloro-6-methylbenzoate

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

Thiede, Sebastian; Wosniok, Paul R.; Herkommer, Daniel; Debnar, Thomas; Tian, Maoqun; Wang, Tongtong; Schrempp, Michael; Menche, Dirk published an article in 2017, the title of the article was Total Synthesis of Leupyrrins A1 and B1, Highly Potent Antifungal Agents from the Myxobacterium Sorangium cellulosum.Name: tert-Butyl trichloroacetimidate And the article contains the following content:

Full details on the design, elaboration, and application of efficient strategies for the high-yielding total syntheses of leupyrrins A1 and B1 (I and II, resp.), unique antifungal agents from the myxobacterium Sorangium cellulosum, are reported. A sequential zirconocene-mediated diyne-cyclization, and regioselective opening of the zirconacyclopentadiene intermediate enabled a concise entry into the unique dihydrofuran fragment, whereas another domino reaction was developed for the butyrolactone involving a one-pot lactol opening, stereoselective aldehyde addition and in situ lactonization. Furthermore, an innovative sp2-sp3-cross-coupling for pyrrole functionalization and an optimized HATU-mediated amide coupling protocol of two elaborate fragments were established. In addition, an unusual protective group strategy, involving a Teoc-acetonide protected amine in combination with tert-Bu and acetate esters, was successfully elaborated. These tactics and strategies are generally useful and may be also applied in the synthesis of other functionalized compounds It is expected that the material which was obtained by these total syntheses will enable the further exploration of the biol. profile of these potent antifungal agents. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Name: tert-Butyl trichloroacetimidate

The Article related to leupyrrin a1 b1 synthesis, zirconocene mediated diyne cyclization regioselective opening zirconacyclopentadiene leupyrrin synthesis, lactol ring opening stereoselective aldehyde addition lactonization leupyrrin synthesis, cross coupling pyrrole functionalization leupyrrin synthesis, hatu mediated amide coupling leupyrrin synthesis and other aspects.Name: tert-Butyl trichloroacetimidate

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

On November 28, 2020, Hawkins, Paige M. E.; Tran, Wendy; Nagalingam, Gayathri; Cheung, Chen-Yi; Giltrap, Andrew M.; Cook, Gregory M.; Britton, Warwick J.; Payne, Richard J. published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Total synthesis and antimycobacterial activity of Ohmyungsamycin A, Deoxyecumicin, and Ecumicin. And the article contained the following:

The ohmyungsamycin and ecumicin natural product families are structurally related cyclic depsipeptides that display potent antimycobacterial activity. Herein the total syntheses of ohmyungsamycin A, deoxyecumicin, and ecumicin are reported, together with the direct biol. comparison of members of these natural product families against Mycobacterium tuberculosis (Mtb), the etiol. agent of tuberculosis (TB). The synthesis of each of the natural products employed a solid-phase strategy to assemble the linear peptide precursor, involving a key on-resin esterification and an optional on-resin dimethylation step, before a final solution-phase macrolactamization between the non-proteinogenic N-methyl-4-methoxy-L-tryptophan amino acid and a bulky N-methyl-L-valine residue. The synthetic natural products possessed potent antimycobacterial activity against Mtb with MIC90’s ranging from 110-360 nM and retained activity against Mtb in Mtb-infected macrophages. Deoxyecumicin also exhibited rapid bactericidal killing against Mtb, sterilizing cultures after 21 days. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to natural product cyclic peptide ohmyungsamycin deoxyecumicin ecumicin total synthesis, cyclopeptide antimycobacterial agent tuberculostatic drug, deoxyecumicin sterilizing agent mycobacterium tuberculosis, solid phase peptide synthesis esterification dimethylation macrolactamization, natural products, peptides, solid-phase synthesis, total synthesis, tuberculosis and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

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