Month: October 2022

Sayago, Francisco J.; Calaza, M. Isabel; Jimenez, Ana I.; Cativiela, Carlos published the artcile< A straightforward route to enantiopure α-substituted derivatives of (2S,3aS,7aS)-octahydroindole-2-carboxylic acid>, Recommanded Product: (2R,3aS,7aS)-Octahydro-1H-indole-2-carboxylic acid, the main research area is indolecarboxylic acid octahydro stereoselective alkylation.

High yielding and remarkably selective alkylations of a suitably protected derivative of (2S,3aS,7aS)-octahydroindole-2-carboxylic acid are described. The fused bicyclic structure of this proline analog greatly influences the stereochem. outcome of direct alkylation reactions taking place at the α-carbon and provides access to α-substituted analogs with retention of the configuration. The overall procedure allows the preparation of enantiopure α-substituted derivatives of this Oic isomer, suitably protected for their incorporation into peptides, in a straightforward manner.

Tetrahedron published new progress about Alkylation, stereoselective. 145513-91-3 belongs to class indole-building-block, and the molecular formula is C9H15NO2, Recommanded Product: (2R,3aS,7aS)-Octahydro-1H-indole-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

Tang, Pan; Wei, You-Yuan; Wen, Long; Ma, Hao-Jie; Yang, Yi; Jiang, Yan published the artcile< MgI2-Catalyzed Nucleophilic Ring-Opening Reactions of Donor-Acceptor Cyclopropanes with Indoline-2-thiones>, COA of Formula: C8H6ClNO, the main research area is gamma indolylthio butyric acid preparation chemoselective magnesium iodide; donor acceptor cyclopropane indoline thione nucleophilic ring opening.

MgI2-catalyzed nucleophilic ring-opening reactions of donor-acceptor cyclopropanes with indoline-2-thiones as easy-to-handle sulfur nucleophiles were investigated. A series of functionalized γ-indolylthio butyric acid derivatives were synthesized in good to excellent yields under mild reaction conditions. Furthermore, the thioether functionalized ring-opening products could be transformed to sulfone and methionine analogs.

Journal of Organic Chemistry published new progress about Chemoselectivity. 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, COA of Formula: C8H6ClNO.

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

Liu, Yuanyuan; Li, Yi; Zong, Linghui; Zhang, Jingyi published the artcile< Comparison of two rhodamine-based polystyrene solid-phase fluorescent sensors for mercury(II) determination>, Application In Synthesis of 950846-89-6, the main research area is rhodamine based polystyrene microsphere fluorescent sensor mercury ion determination.

Two novel rhodamine-based polystyrene solid-phase fluorescent sensors PS-AC-I and PS-AC-II with different coordination atoms (O or S) are synthesized and shown to be able to detect Hg(II) ions. They are characterized by Fourier-transform IR spectroscopy and by SEM anal. Their fluorescent properties, including response time, pH effects, fluorescence titrations, metal ion competition and recycling, are investigated and compared. Sensor PS-AC-II displayed higher selectivity and sensitivity to Hg(II), with a lower detection limit of 0.032μM, which was 15 times better than PS-AC-I. A detection mechanism involving the Hg(II) chelation-induced ring-opening of the rhodamine spirolactam is proposed with the aid of theor. calculations

Journal of Chemical Research published new progress about Fluorescence. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Application In Synthesis of 950846-89-6.

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

Adak, Arup Kumar; Dutta, Basudeb; Manna, Saikat Kumar; Sinha, Chittaranjan published the artcile< Rhodamine-Appended Benzophenone Probe for Trace Quantity Detection of Pd2+ in Living Cells>, Quality Control of 950846-89-6, the main research area is rhodamine benzophenone palladium living cell.

Designing a fluorogenic probe for the determination of Pd2+ is a challenging anal. task. Pd2+ is a potentially toxic and harmful substance even at a very low level of contamination in the end product. Herein, a promising spirolactam-functionalized chemosensor, rhodamine-appended benzophenone (HBR), is designed and characterized by spectroscopic (1H NMR, 13C NMR, ESI-MS, and FT-IR) data along with the single-crystal x-ray diffraction technique. It acts as a highly sensitive and selective fluorogenic chemosensor for Pd2+ ions over other environmentally relevant cations in aqueous ethanol (1:1, volume/volume) at pH 7.4. The limit of detection (LOD) is 34 nM that is far below the WHO recommended Pd uptake (47μM). The plausible mechanism involves the specific binding of HBR with Pd2+ and the formation of 1:1 stoichiometry of the complex, which has been supported by ESI-MS, FT-IR data, Job plot, and association constant data (Benesi-Hildebrand plot). The computation study has been attempted to explain the ring cleavage fluorescence enhancement scheme of HBR upon binding with Pd2+. Furthermore, this “”turn-on”” probe has successfully applied to image the Pd2+ ion in cultured MDA-MB-231 cells.

ACS Omega published new progress about Fluorescence spectroscopy. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Quality Control of 950846-89-6.

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

Prasad, Bagineni; Das, Rabindra Nath; Jamroskovic, Jan; Kumar, Rajendra; Hedenstroem, Mattias; Sabouri, Nasim; Chorell, Erik published the artcile< The relation between position and chemical composition of bis-indole substituents determines their interactions with G-quadruplex DNA>, Safety of Methyl 1H-indole-7-carboxylate, the main research area is human DNA G quadruplex sidechain bis indole drug target; DNA structures; G-Quadruplexes; bis-indole; drug design; nitrogen heterocycles.

G-quadruplex (G4) DNA structures are linked to fundamental biol. processes and human diseases, which has triggered the development of compounds that affect these DNA structures. However, more knowledge is needed about how small mols. interact with G4 DNA structures. This study describes the development of a new class of bis-indoles (3,3-diindolyl-Me derivatives) and detailed studies of how they interact with G4 DNA using orthogonal assays, biophys. techniques, and computational studies. This revealed compounds that strongly bind and stabilize G4 DNA structures, and detailed binding interactions which for example, show that charge variance can play a key role in G4 DNA binding. Furthermore, the structure-activity relationships generated opened the possibilities to replace or introduce new substituents on the core structure, which is of key importance to optimize compound properties or introduce probes to further expand the possibilities of these compounds as tailored research tools to study G4 biol.

Chemistry – A European Journal published new progress about Animal gene, c-myc Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, Safety of Methyl 1H-indole-7-carboxylate.

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

Tan, Zhi-Yu; Wu, Ke-Xin; Huang, Lu-Shan; Wu, Run-Shi; Du, Zheng-Yu; Xu, Da-Zhen published the artcile< Iron-catalyzed cross-dehydrogenative coupling of indolin-2-ones with active methylenes for direct carbon-carbon double bond formation>, Electric Literature of 20870-77-3, the main research area is indolinone active methylene iron cross dehydrogenative coupling green; alkene preparation.

The iron-catalyzed cross-dehydrogenative coupling (CDC) of C(sp3)-H/C(sp3)-H bonds to afford olefins by 4H elimination is described. This method employs air (mol. oxygen) as an ideal oxidant, and is performed under mild, ligand-free and base-free conditions. H2O is the only byproduct. Good tolerance of functional groups and high yields have also been achieved. Preliminary mechanistic investigations suggest that the present transformation involves a radical process.

Green Chemistry published new progress about Active methylene compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Electric Literature of 20870-77-3.

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

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