Day: October 12, 2022

Chen, Lili; Shen, Jun-Jian; Gao, Qian; Xu, Senmiao published the artcile< Synthesis of cyclic chiral α-amino boronates by copper-catalyzed asymmetric dearomative borylation of indoles>, Product Details of C9H6FNO2, the main research area is cyclic chiral alpha amino boronate preparation; copper catalyzed asym dearomative borylation indole; borylindoline enantioselective preparation crystal mol structure.

A copper(I)-catalyzed dearomative borylation of N-alkoxycarbonyl protected indole-3-carboxylates has been developed. The boron addition in this reaction occurred regioselectively at the 2-position of indoles followed by diastereoselective protonation, affording the corresponding stable cyclic chiral α-amino boronates (2-borylindolines) in moderate to good yields with excellent diastereo- and enantioselectivities. The product 2c could be used as a versatile precursor to undergo subsequent stereoselective transformations, delivering highly functionalized 2,3,3-trisubstituted chiral indolines.

Chemical Science published new progress about Borylation (dearomative). 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Product Details of C9H6FNO2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Sawama, Yoshinari; Nakano, Akihiro; Matsuda, Takumi; Kawajiri, Takahiro; Yamada, Tsuyoshi; Sajiki, Hironao published the artcile< H-D Exchange Deuteration of Arenes at Room Temperature>, Recommanded Product: 5-Fluoroindole-2-carboxylic acid, the main research area is deuterated arene chemoselective preparation; platinum iridium catalyst deuteration arene deuterium oxide under argon.

Arenes underwent C-H deuteration reactions with D2O in the presence of Pt/C, Ir/C, or combinations of both catalysts in isopropanol/D2O under argon at ambient temperature to yield arenes deuterated at the arene C-H bonds.

Organic Process Research & Development published new progress about Aromatic hydrocarbons Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Recommanded Product: 5-Fluoroindole-2-carboxylic acid.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Gopalaiah, Kovuru; Tiwari, Ankit published the artcile< Synthesis of (E)-3-Alkylideneindolin-2-ones by an Iron-Catalyzed Aerobic Oxidative Condensation of Csp3-H Bonds of Oxindoles and Benzylamines>, Safety of 4-Chloroindolin-2-one, the main research area is alkylideneindolinone preparation iron catalyst oxidative condensation oxindole benzylamine.

A novel synthetic route for the construction of (E)-3-alkylideneindolin-2-ones through iron-catalyzed aerobic oxidative condensation of oxindoles with benzylamines was developed. This oxidative reaction involves a sequence of C-H activation, amine self-condensation, nucleophilic addition, and C-C double bond formation. The synthetic importance of this protocol was demonstrated by preparing tyrosine kinase inhibitors, anticonvulsant and antitumor agents, and other valuable 3-alkylideneindolin-2-one derivatives Key intermediates were isolated and a plausible mechanistic pathway for the reaction is discussed.

European Journal of Organic Chemistry published new progress about Aralkyl amines Role: RCT (Reactant), RACT (Reactant or Reagent). 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Safety of 4-Chloroindolin-2-one.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Nirogi, Ramakrishna; Gagginapally, Shankar Reddy; Shinde, Anil K.; Mohammed, Abdul Rasheed published the artcile< Synthesis of GR125487, a selective 5-HT4 receptor antagonist>, HPLC of Formula: 23077-43-2, the main research area is GR125487 synthesis serotonin receptor 5HT4 antagonist cognition.

The 5-HT4 receptor (5-HT4R) agonists are important in treating gastrointestinal motility disorders. Their role is currently being evaluated for the treatment of cognitive and mood disorders. A selective 5-HT4R antagonist GR 125487 is used in many biol. assays to cross confirm the 5-HT4R agonist’s activity. A practical synthesis of GR 125487 is developed so as to have it in desired quantities. The synthesis consists of seven steps starting from com. available Me 5-fluoroindole 3-carboxylate. The GR 125487 thus synthesized was used in blocking the activity of 5-HT4R agonist compound in animal models of cognition.

Synthetic Communications published new progress about 5-HT4 agonists. 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, HPLC of Formula: 23077-43-2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Lei; Fang, Kun; Cheng, Junfei; Li, Yu; Huang, Yahui; Chen, Shuqiang; Dong, Guoqiang; Wu, Shanchao; Sheng, Chunquan published the artcile< Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer>, Application In Synthesis of 399-76-8, the main research area is colon cancer antitumor agents SAR topoisomerase tubulin scaffold apoptosis.

Inspired by the natural product evodiamine, a novel antitumor indolopyrazinoquinazolinone scaffold was designed by scaffold hopping. Structure-activity relationship studies led to the discovery of compound 15j, which shows low nanomolar inhibitory activity against the HCT116 cell line. Further antitumor mechanism studies indicated that compound 15j acted by the dual inhibition of topoisomerase 1 and tubulin and induced apoptosis with G2 cell-cycle arrest. The quaternary ammonium salt of compound 15j (compound 15js) exhibited excellent in vivo antitumor activity (TGI = 66.6%) in the HCT116 xenograft model with low toxicity. Indolopyrazinoquinazolinone derivatives represent promising multitargeting antitumor leads for the development of novel antitumor agents.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Application In Synthesis of 399-76-8.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Xing, Siyang; Guo, Junsuo; Wang, Yuhan; Wang, Chenyu; Wang, Kui; Zhu, Bolin published the artcile< General and efficient synthesis of 1,2-dihydropyrrolo[3,4-b]indol-3-ones via a formal [3 + 2] cycloaddition initiated by C-H activation>, Product Details of C10H9NO, the main research area is dihydropyrroloindolone preparation; isocyanate indole cycloaddition rhodium catalyst.

A [Cp*RhCl2]2-catalyzed formal [3 + 2] cycloaddition between isocyanates and indoles with electron-deficient alkenes at the C3-position of the indole moiety and directing groups at the N1-position of the indole moiety was described. Undergoing sequential coupling reaction initiated by C-H activation and aza-Michael addition, a series of 1,2-dihydropyrrolo[3,4-b]indol-3-ones I [R = Et, n-Bu, Bn, etc.; R1 = CO2Et, CO2Me, etc.; R2 = H, F, Cl, etc.; R3 = H, F, Br, etc.; R4 = H, Me, F, etc.; R5 = H, Me] was successfully afforded in moderate to good yields by the formation of one C-C bond and one C-N bond. Interestingly, the pyridyl group at the N1-position of the indole moiety not only played a role as the directing group, but also catalyzed further intramol. Michael addition as a base.

Organic Chemistry Frontiers published new progress about C-H bond activation. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Product Details of C10H9NO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Yu, Hui-juan; Zhao, Wei; Xie, Mengting; Li, Xiaoqing; Sun, Ming; He, Jun; Wang, Lu; Yu, Lin published the artcile< Real-Time Monitoring of Self-Aggregation of β-Amyloid by a Fluorescent Probe Based on Ruthenium Complex>, Formula: C9H6FNO2, the main research area is self aggregation beta amyloid ruthenium complex fluorescent imaging.

Self-accumulation of amyloid-β protein (Aβ) into insoluble fibrils is the major hallmark of Alzheimer’s disease. Real-time monitoring of fibril growth is essential for clarifying the mechanism underlying aggregation and discovering therapeutic targets. A variety of approaches including NMR, electron microscopy (EM), at. force microscopy (AFM), and total internal reflection fluorescence microscopy (TIRFM) have been explored to monitor the fibril growth or reveal morphol. of Aβ aggregates. However, none of the methods allow real-time observation under physiol. conditions while without any perturbations. Here, the authors present a fluorescent probe [Ru(phen)2(fipc)]2+ (Ru-fipc) (phen = 1,10-phenanthroline, fipc = 5-fluoro-N-(1,10-phenanthrolin-5-yl)-1H-indole-2-carboxamide) that can bind to all the Aβ forms, i.e., monomers, oligomers, and fibrils, while not perturbing aggregation. Using this probe in combination with laser confocal microscopy, the entire aggregation process could be clearly and exactly imaged at the single fibril level. The reliability of Ru-fipc was confirmed based on colocalization with thioflavin T (ThT). Importantly, Ru-fipc can be used to monitor the very early nucleation and oligomerization process, which is thought to be a critical step in the development of neurotoxicity while it cannot be visualized with ThT. To the knowledge, this is the first fluorescent probe developed for real-time monitoring of Aβ aggregation, especially for the very early assembly stage, in solution with minimal perturbation. This method is suitable for in vitro and in vivo studies. The authors believe this would provide a valuable complementary tool for the study of pathogenesis and discovery of therapeutic targets of neurodegenerative diseases.

Analytical Chemistry (Washington, DC, United States) published new progress about Confocal laser scanning microscopy. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Formula: C9H6FNO2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Harada, Hiroshi; Hirokawa, Yoshimi; Suzuki, Kenji; Hiyama, Yoichi; Oue, Mayumi; Kawashima, Hitoshi; Yoshida, Naoyuki; Furutani, Yasuji; Kato, Shiro published the artcile< Novel and potent human and rat β3-adrenergic receptor agonists containing substituted 3-indolylalkylamines>, Name: 4-Methyl-1H-indole-3-carbaldehyde, the main research area is indolylalkylamine preparation adrenergic agonist.

A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanols was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human β3-adrenergic receptor (AR). The optically active I was found to be the most potent and selective human β3-AR agonist in this series with an EC50 value of 0.062 nM. In addition, the selectivity of I for human β3-AR was 210-fold and 103-fold that for human β2-AR and β1-AR, resp. Furthermore, I showed potent agonistic activity at rat β3-AR.

Bioorganic & Medicinal Chemistry Letters published new progress about Aryl aldehydes, heteroaryl Role: RCT (Reactant), RACT (Reactant or Reagent). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Name: 4-Methyl-1H-indole-3-carbaldehyde.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Kredel, Julia; Gallei, Markus published the artcile< Ozone-Degradable Fluoropolymers on Textile Surfaces for Water and Oil Repellency>, Formula: C30H36N4O2, the main research area is ozone degradable fluoropolymer textile surfaces water oil repellency.

Resistant and functional coatings on surfaces have been of growing interest recently. Functional textiles featuring water- and oil-repellent properties can be achieved by convenient coating of textiles with highly fluorinated polymers. Recently, concerns about (per)fluorinated mols. have been reported due to the high persistence and accumulation capabilities in nature, driving the textile market to develop alternatives and novel strategies. Within this study an ozone-degradable fluorinated polymer for water and oil repellency on various textiles is reported. The monomer 2-((1,1,2-trifluoro-2-(perfluoropropoxy)ethyl)thio)ethyl acrylate is capable of side-chain degradation upon ozone treatment due to the presence of chem. cleavable moieties. The degradable fluorine-containing polymer is accessible via radical polymerization in emulsion polymerization and can be directly applied onto various textiles, e.g., polyamide, polyester, Nomex, or cotton, by using a foulard. To investigate the homogeneous coating performance on the resp. textiles, a model polymer featuring a fluorescent monomer as part of the polymer chain is prepared, enabling the investigation of the polymer distribution via confocal microscopy. Finally, the effect of the fluorine moieties and the molar mass of the polymers is investigated, and the ozone-induced degradation is elucidated. The herein-described fluorinated polymers are envisaged to be a promising and nonpersistent platform for the preparation of omniphobic textile coating.

ACS Applied Polymer Materials published new progress about Cellulose pulp. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Formula: C30H36N4O2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Zhao-Yang; Guo, Rui-Li; Zhang, Xing-Long; Wang, Meng-Yue; Chen, Gang-Ni; Wang, Yong-Qiang published the artcile< Regioselective C5-H direct iodination of indoles>, COA of Formula: C10H9NO, the main research area is iodo indole regioselective preparation; aryl iodide iodosuccinimide iodination.

An efficient regioselective C5-H direct iodination of indoles I [R = H, 6-Cl, 4-Me, etc.; R1 = C(O)H, CN, C(O)OMe, C(O)OEt] was developed for the first time. Due to the versatility of aryl iodides, the method offered a general and practical access to the C5 functionalization of indoles. The approach featured mild reaction conditions, good tolerance of functional groups and more crucially, no metal involved in the reaction, thereby benefitting the late-stage decoration of medicinal mols. A mechanistic study showed that the current iodination reaction proceeded via a radical pathway.

Organic Chemistry Frontiers published new progress about Aryl iodides Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, COA of Formula: C10H9NO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles