Category: 13523-93-8

Gao, Mingzhang published the artcileSynthesis of carbon-11-labeled 4-aryl-4H-chromenes as new PET agents for imaging of apoptosis in cancer, Name: 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is arylbenzopyrancarbonitrile carbon 11 preparation PET imaging apoptosis.

Carbon-11-labeled 4-aryl-4H-chromenes, 4-(3-[11C]methoxy-5-methoxyphenyl)-, 4-(3-bromo-4-[11C]methoxy-5-methoxyphenyl)-, 4-(3-[11C]methoxy-5-methoxyphenyl)-, 4-(3-bromo-4-[11C]methoxy-5-methoxyphenyl)-, 4-(3-[11C]methoxy-5-methoxyphenyl)-, 4-(3-bromo-4-[11C]methoxy-5-methoxyphenyl)-, 4-(3-[11C]methoxy-5-methoxyphenyl)- and 4-(3-bromo-4-[11C]methoxy-5-methoxyphenyl)–2-amino-7-methyl-4,7-dihydropyrano[2,3-e]indole-3-carbonitrile were prepared by O-[11C]methylation of their alc. precursors using [11C]CH3OTf under basic conditions and isolated by a simplified solid-phase extraction (SPE) method in 30-50% radiochem. yields based on [11C]CO2 and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 15-20 min, the radiochem. purity was >99%, and the specific activity at end of synthesis (EOS) was 111-185 GBq/μmol.

Applied Radiation and Isotopes published new progress about Apoptosis. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Name: 4-(Benzyloxy)-1-methyl-1H-indole.

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

Corrieri, Matteo published the artcilePractical and sustainable preparation of pyrrolo[2,3-b]indoles by Cu/Fe catalyzed intramolecular C(sp2)-H amination, Name: 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is pyrrolo indole copper iron catalyzed intramol amination.

A practical, robust and chemoselective approach toward the synthesis of pyrrolo[2,3-b]indoles via direct intramol. C-H bond amination of α-indolylhydrazones has been achieved. This base- and oxidant-free chemoselective transformation relies on a Cu/Fe co-catalyst system that operates at 50 °C in air with water as the only reaction medium. The easy product isolation together with the recyclable catalyst aqueous system (reused at least five times, maintaining over 50% of its catalytic activity) can provide an effective environmentally benign approach to fused N-heterocycles of remarkable interest in pharmaceutical and medicinal chem. The ability of the hydrazone residue to act as a chelating/directing group as well as an aminating agent guarantees the success of this C-H functionalization.

Green Chemistry published new progress about Amination. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Name: 4-(Benzyloxy)-1-methyl-1H-indole.

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

Qin, Qixue published the artcileVisible-Light-Promoted Redox Neutral C-H Amidation of Heteroarenes with Hydroxylamine Derivatives, Name: 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is iridium photocatalyst amidation heteroarene hydroxylamine derivative.

A room temperature redox neutral direct C-H amidation of heteroarenes has been achieved. Hydroxylamine derivatives, which are easily accessed, have been employed as tunable nitrogen sources. These reactions were enabled by a visible-light-promoted single-electron transfer pathway without a directing group. A variety of heteroarenes, such as indoles, pyrroles, and furans, could go through this amidation with high yields (up to 98%). E.g., irradiation of N-methylindole, TsONTsMe, the photocatalyst fac-Ir(ppy), and NaHCO3 in DMF gave 66% amide (I). These reactions are highly regioselective, and all the products were isolated as a single regioisomer.

Organic Letters published new progress about Amidation. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Name: 4-(Benzyloxy)-1-methyl-1H-indole.

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, Weidong published the artcileCatalytic Aerobic Dehydrogenation of N-Heterocycles by N-Hydoxyphthalimide, Application In Synthesis of 13523-93-8, the main research area is indole preparation; indoline dehydrogenation hydoxyphthalimide catalyst; quinoline preparation; tetrahydroquinolinine aerobic dehydrogenation hydoxyphthalimide catalyst copper.

Catalytic methods for the aerobic dehydrogenation of N-heterocycles were reported. In most cases, indoles were accessed efficiently from indolines using catalytic N-hydroxyphthalimide (NHPI) as the sole additive under air. For more challenging substrates and to expand the scope to other heterocycles, a catalyst system of NHPI and copper was developed.

Advanced Synthesis & Catalysis published new progress about Dehydrogenation. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Application In Synthesis of 13523-93-8.

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

Li, Laiqiang published the artcileSite-Selective Electrochemical C-H Cyanation of Indoles, COA of Formula: C16H15NO, the main research area is carbonitrile indole green regioselective preparation; indole trimethylsilyl cyanide electrochem cyanation tris bromophenyl amine catalyst.

An electrochem. approach for the site-selective C-H cyanation of indoles to form indole-carbonitriles I [R1 = CN, Ph; R2 = Me, CN, C(O)OMe, etc.; R3 = H, 4-Me, 5-F, 6-Cl, etc.; R4 = Me, Bn, i-Pr, etc.] employing readily available TMSCN as cyano source has been developed. The electrosynthesis relied on the tris(4-bromophenyl)amine as a redox catalyst, which achieved better yield and regioselectivity. A variety of C2- and C3-cyanated indoles were obtained in satisfactory yields. The reactions were conducted in a simple undivided cell at room temperature and obviated the need for transition-metal reagent and chem. oxidant.

Organic Letters published new progress about Cyanation (C-H). 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, COA of Formula: C16H15NO.

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

Kemnitzer, William published the artcileDiscovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions, Application of 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is aryl chromene preparation structure antitumor neoplasm.

In the continuing effort to discover and develop apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, the authors explored the structure-activity relationship (SAR) of alkyl substituted pyrrole fused at the 7,8-positions. A Me group substituted at the nitrogen in the 7-position of the pyrrole ring led to a series of potent apoptosis inducers with potency in the low nanomolar range. These compounds were also found to be low nanomolar or subnanomolar inhibitors of cell growth, and they inhibited tubulin polymerization, indicating that methylation of the 7-position nitrogen does not change the mechanism of action of these chromenes. Compound 2 d was identified as a highly potent apoptosis inducer with an EC50 value of 2 nM and a highly potent inhibitor of cell growth with a GI50 value of 0.3 nM in T47D cells.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Application of 4-(Benzyloxy)-1-methyl-1H-indole.

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

Li, Xiang published the artcileAerobic Transition-Metal-Free Visible-Light Photoredox Indole C-3 Formylation Reaction, Quality Control of 13523-93-8, the main research area is indole TMEDA oxygen Rose Bengal visible light photoredox formylation; formyl indole regioselective preparation.

An aerobic visible-light-promoted indole C-3 formylation reaction catalyzed by Rose Bengal has been developed. This transition-metal-free process employs mol. oxygen as the terminal oxidant and uses TMEDA as the one-carbon source through C-N bond cleavage. The reaction is compatible with a variety of functional groups.

ACS Catalysis published new progress about C-N bond cleavage. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Quality Control of 13523-93-8.

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

Tong, Kun published the artcileVisible-Light-Induced Direct Oxidative C-H Amidation of Heteroarenes with Sulfonamides, Related Products of indole-building-block, the main research area is heterocyclic compound preparation regioselective photochem; heteroarene sulfonamide oxidative carbon hydrogen amidation iridium catalyst; C−H amidation; heterocycles; nitrogen-centered radicals; photochemistry; visible light.

A direct oxidative C-H amidation of heteroarenes, e.g., I, with sulfonamides RNHSO2R1 [R = CH3, C6H5, oxan-4-yl, etc.; R1 = CH3(CH2)4, C6H5, c-C3H5, pyridin-3-yl, etc.] via nitrogen-centered radicals has been described. Nitrogen-centered radicals are directly generated from oxidative cleavage of NH bonds under visible-light photoredox catalysis. Sulfonamides, which are easily accessed, used as tunable nitrogen sources. Bleach (aqueous NaClO solution), which is clean and economic, was used as the solely oxidant. A variety of heteroarenes, including indoles, pyrroles, and benzofurans, can undergo this amidation with high yields (up to 92%). These reactions are highly regioselective, and all the products, e.g., II, are isolated as single regioisomer.

Chemistry – A European Journal published new progress about Amidation (regioselective). 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Related Products of indole-building-block.

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

Jiang, Zhigan published the artcileScaffold hopping of sampangine: discovery of potent antifungal lead compound against Aspergillus fumigatus and Cryptococcus neoformans, Recommanded Product: 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is antifungal sampangine derivative; Antifungal activity; Sampangine; Scaffold hopping.

Discovery of novel antifungal agents against Aspergillus fumigatus and Cryptococcus neoformans remains a significant challenge in current antifungal therapy. Here, the antifungal natural product sampangine (I) was used as the lead compound for novel antifungal drug discovery. D-ring scaffold hopping derivatives were designed and synthesized to improve antifungal activity and water solubility Among them, the thiophene derivative S2 showed broad-spectrum antifungal activity, particularly for Aspergillus fumigatus and Cryptococcus neoformans. Moreover, compound S2 also revealed better water solubility than sampangine, which represents a promising antifungal lead compound for further structural optimization.

Bioorganic & Medicinal Chemistry Letters published new progress about Aspergillus fumigatus. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Recommanded Product: 4-(Benzyloxy)-1-methyl-1H-indole.

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

Liang, Taoyuan published the artcileStraightforward access to novel indolo[2,3-b]indoles via aerobic copper-catalyzed [3+2] annulation of diarylamines and indoles, HPLC of Formula: 13523-93-8, the main research area is diarylamino indoloindole chemoselective preparation; diarylamine indole aerobic annulation copper catalyst.

An unprecedented aerobic copper-catalyzed [3+2] annulation reaction of diarylamines with indoles was reported, which allowed direct access to novel 2-diarylamino-indolo[2,3-b]indoles I [R = Ph, 4-MeC6H4, 4-ClC6H4, etc.; R1 = Me, Et, Bn, etc.; R2 = H, 4-Me, 6-F, etc.; Ar = Ph, 4-MeC6H4, 4-t-BuC6H4, etc.; Ar1 = Ph, 4-MeC6H4], a class of potential photoelec. device mols. The developed transformation proceeded with broad substrate scope, good functional group tolerance, high chemo-selectivity and no need for pre-preparation of specific agents, which offered a practical route for diverse and atom-economic synthesis of the desired products.

Chemical Communications (Cambridge, United Kingdom) published new progress about [3+2] Cycloaddition reaction. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, HPLC of Formula: 13523-93-8.

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