Category: 41910-64-9

Yao, Chun-Hsu published the artcileDiscovery of Novel N-β-D-Xylosyl-indole Derivatives as Sodium-Dependent Glucose Co-transporter 2 (SGLT2) Inhibitors for the Management of Hyperglycemia in Diabetes, SDS of cas: 41910-64-9, the main research area is aryl C glycoside preparation antidiabetic; human xyloside indole SGLT2 inhibitor hyperglycemia diabetes antidiabetic preparation.

A novel series of N-linked β-D-xylosides were synthesized and evaluated for inhibitory activity against sodium-dependent glucose co-transporter 2 (SGLT2) in a cell-based assay. Of these, the β-D-xylopyranosyl-1H-indole I (R = 4-chlorocyclopropylbenzyl) was the most potent inhibitor, with an EC50 value similar to that of the natural SGLT2 inhibitor phlorizin. Further studies in Sprague-Dawley (SD) rats indicated that I significantly increased urine glucose excretion in a dose-dependent manner with oral administration. The antihyperglycemic effect of I was also observed in streptozotocin (STZ) induced diabetic SD rats. These results described here are a good starting point for further investigations into N-glycoside SGLT2 inhibitors.

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, SDS of cas: 41910-64-9.

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

Zhang, Hailong published the artcileConstruction of the N1-C3 Linkage Stereogenic Centers by Catalytic Asymmetric Amination Reaction of 3-Bromooxindoles with Indolines, Product Details of C8H8ClN, the main research area is nickel catalyst asym amination bromooxindole indoline.

The catalytic asym. amination reaction of 3-bromooxindoles with indolines for the construction of the N1-C3 linkage stereogenic centers has been realized for the first time. E.g., in presence of Ni(OAc)2, ligand (I), and DABCO in MTBE, amination of 3-bromooxindole derivative (II) with indoline gave 87% III. Moreover, the racemic substrates (3-substituted indolines) were also applicable under the same chiral conditions. The newly developed method conveniently led to a formal synthesis of (+)-psychotrimine.

Organic Letters published new progress about Amination catalysts. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Product Details of C8H8ClN.

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

Zhao, He published the artcileIndoline and piperazine containing derivatives as a novel class of mixed D2/D4 receptor antagonists. Part 1: Identification and structure-activity relationships, SDS of cas: 41910-64-9, the main research area is dopamine receptor antagonist indoline piperazine derivative preparation SAR.

Optimization of the lead compound 2-[-4-(4-chlorobenzyl)piperazin-1-yl]-1-(2,3-dihydroindol-1-yl)ethanone by systematic structure-activity relation (SAR) studies leads to two potent compounds 2-[-4-(4-chlorobenzyl)piperazin-1-yl]-1-(2-methyl-2,3-dihydroindol-1-yl)ethanone and 2-[-4-(4-chlorobenzyl)piperazin-1-yl]-1-(2-methy-2,3-dihydroindol-1-yl)ethanone. Synthesis and structure-activity relationship as mixed D2/D4 receptor antagonists are reported.

Bioorganic & Medicinal Chemistry Letters published new progress about Dopamine D2 antagonists. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, SDS of cas: 41910-64-9.

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

Dong, Yanan published the artcileReductive cyanation of organic chlorides using CO2 and NH3 via Triphos-Ni(I) species, Application In Synthesis of 41910-64-9, the main research area is nitrile preparation; chloride organic reductive cyanation.

The reductive cyanation of organic chlorides RCl (R = C6H5, naphthalen-1-yl, cyclohexyl, etc.) using CO2/NH3 as the electrophilic CN source has been described. The use of tridentate phosphine ligand Triphos allows for the nickel-catalyzed cyanation of a broad array of aryl and aliphatic chlorides to produce the desired nitrile products RCN in good yields, and with excellent functional group tolerance. Cheap and bench-stable urea was also shown as suitable CN source, suggesting promising application potential. Mechanistic studies imply that Triphos-Ni(I) species are responsible for the reductive C-C coupling approach involving isocyanate intermediates. This method expands the application potential of reductive cyanation in the synthesis of functionalized nitrile compounds under cyanide-free conditions, which is valuable for safe synthesis of (isotope-labeled) drugs.

Nature Communications published new progress about Antiproliferative agents. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Application In Synthesis of 41910-64-9.

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

Saczewski, Franciszek published the artcile1-[(Imidazolin-2-yl)amino]indoline and 1-[(imidazolin-2-yl)amino]1,2,3,4-tetrahydroquinoline derivatives: new insights into their circulatory activities, Category: indole-building-block, the main research area is imidazolinylamino indoline hydrochloride preparation mol modeling imidazoline adrenoceptor antihypertensive; quinoline imidazolinylamino hydrochloride preparation mol modeling imidazoline adrenoceptor antihypertensive.

N-[(Imidazolinyl)amino]indoline-hydrochlorides I·HCl [R = H, 2-CH3, 7-CH3, 4-Cl] and N-[(imidazolinyl)amino]tetrahydroquinoline-hydrochlorides II·HCl [R = H, 8-CH3] were synthesized and tested in vitro for their affinities to α1 and α2-adrenoceptors as well as imidazoline I1 and I2 receptors. The compounds most potent at either α1 or α2-adrenoceptors were administered i.v. to normotensive Wistar rats to determine their effects on mean arterial blood pressure and heart rate. Upon i.v. administration at dose of 0.1 mg/kg to normotensive male Wistar rats, the initial transient pressor effect was followed by long-lasting hypotension and bradycardia. The results revealed that the synthesized compounds I and II were found to possess circulatory profile characteristic of the centrally acting clonidine-like hypotensive imidazolines.

Acta Poloniae Pharmaceutica published new progress about Adrenoceptor antagonists. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Category: 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

Zhao, Fei published the artcileMonoamine Oxidase (MAO-N) Biocatalyzed Synthesis of Indoles from Indolines Prepared via Photocatalytic Cyclization/Arylative Dearomatization, Application In Synthesis of 41910-64-9, the main research area is monoamine oxidase indole indoline photocatalytic cyclization dearomatization.

The biocatalytic aromatization of indolines into indole derivatives exploiting monoamine oxidase (MAO-N) enzymes is presented. Indoline substrates were prepared via photocatalytic cyclization of arylaniline precursors or via arylative dearomatization of unsubstituted indoles and in turn chemoselectively aromatized by the MAO-N D11 whole cell biocatalyst. Computational docking studies of the indoline substrates in the MAO-N D11 catalytic site allowed for the rationalization of the biocatalytic mechanism and exptl. results of the biotransformation. This methodol. represents an efficient example of biocatalytic synthesis of indole derivatives and offers a facile approach to access these aromatic heterocycles under mild reaction conditions.

ACS Catalysis published new progress about Biotransformation (whole-cell). 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Application In Synthesis of 41910-64-9.

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

Xiong, Dan published the artcileRhodium-Catalyzed Mild C7-Amination of Indolines with Nitrosobenzenes, COA of Formula: C8H8ClN, the main research area is pyrimidinyl indoline nitrosobenzene rhodium catalyst regioselective amination reaction; phenylamino indolinone preparation green chem crystal structure.

A mild and practical Rh(III)-catalyzed C7-H amination of indolines were described, which allows the synthesis of a variety of 7-amino-substituted indolines with good functional group tolerance and high atom economy. Notably, nitrosobenzenes served as nitrogen source in this transformation, and therefore behave environmentally friendly for C-N bond constructions.

ChemistrySelect published new progress about Amination catalysts (regioselective). 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, COA of Formula: C8H8ClN.

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

Yang, Xiao-Hui published the artcileIntermolecular Hydroamination of 1,3-Dienes To Generate Homoallylic Amines, Name: 4-Chloroindoline, the main research area is rhodium catalyzed intermol hydroamination diene Bronsted acid BINAP effect; homoallylic amine preparation anti Markovnikov selectivity.

Authors report a Rh-catalyzed hydroamination of 1,3-dienes to generate homoallylic amines. The work show-cases the first case of anti-Markovnikov selectivity in the intermol. coupling of amines and 1,3-dienes. By tuning the ligand properties and Bronsted acid additive, it was found that a combination of rac-BINAP and mandelic acid is critical for achieving anti-Markovnikov selectivity.

Journal of the American Chemical Society published new progress about Addition reaction (anti-Markovnikov). 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Name: 4-Chloroindoline.

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

Rae, James published the artcileSynthesis of Axially Chiral C-N Scaffolds via Asymmetric Coupling with Enantiopure Sulfinyl Iodanes, Recommanded Product: 4-Chloroindoline, the main research area is copper catalyzed atropselective coupling chiral iodane sulfoxide auxiliary; axially chiral carbon nitrogen scaffold synthesis.

Axially chiral C-N compounds are an emerging but scarcely investigated class of stereogenic mols. with potential applications as biol. active scaffolds and chiral ligands. The synthesis of these compounds is extremely challenging, and in particular, no metal-catalyzed asym., intermol. C-N coupling has been previously reported. Herein we disclose an intermol. atropselective C-N coupling, occurring with excellent stereoselectivity. This Cu-catalyzed transformation is based on the use of highly active coupling partners (i.e., chiral iodanes bearing a very cheap and traceless sulfoxide auxiliary). Use of such original ortho-sulfoxide iodanes enables this unprecedented coupling to occur at room temperature, guaranteeing high atropselectivity and atropselectivity of the coupling products under reaction conditions. Because of extensive possible postmodifications of the optically pure products, a panel of C-N axially chiral scaffolds can now be accessed.

ACS Catalysis published new progress about Anion exchange (of sulfoxide iodanes). 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Recommanded Product: 4-Chloroindoline.

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

Yang, Yurong published the artcileRu(II)-Catalyzed and acidity-controlled tunable [5+1]/[5+2] annulation for building ring-fused quinazolines and 1,3-benzodiazepines, Product Details of C8H8ClN, the main research area is indolyl benzimidazole preparation propargyl carbonate ruthenium catalyst regioselective cycloaddition; isobutenyl benzoimidazopyrroloquinazoline preparation; alkenyl benzoimidazodiazepinoindole preparation.

The Ru(II)-catalyzed tunable [5+1]/[5+2] annulation of N-benzo[d]imidazole indolines with propargyl carbonates was realized for the divergent synthesis of ring-fused quinazolines and 1,3-benzodiazepines bearing various functional groups. These transformations represented an efficient and practical strategy in constructing complex heterocycles via diversified C-H functionalization. A distinctive acidity-controlled reaction manner was clarified to account for the chemoselectivity.

Chemical Communications (Cambridge, United Kingdom) published new progress about [5+2] Cycloaddition reaction (regioselective). 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Product Details of C8H8ClN.

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