Category: 57663-18-0

Lillich, Felix F. published the artcileStructure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors, Safety of Methyl 2-methyl-1H-indole-5-carboxylate, the main research area is antitumor structure activity relationship epoxide hydrolase inhibitor.

A dual partial PPARγ agonist/sEH inhibitor using a structure-guided approach was designed. Exhaustive structure-activity relationship studies lead to the successful optimization of the designed lead. Crystal structures of one representative compound with both targets revealed potential points for optimization. The optimized compounds exhibited favorable metabolic stability, toxicity, selectivity, and desirable activity in adipocytes and macrophages.

Journal of Medicinal Chemistry published new progress about Adipocyte, preadipocyte. 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Safety of Methyl 2-methyl-1H-indole-5-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

Knepper, Kerstin published the artcileBartoli Indole Synthesis on Solid Supports, HPLC of Formula: 57663-18-0, the main research area is indolecarboxylate Bartoli synthesis solid phase.

Bartoli indole synthesis was performed on solid supports. Starting from Merrifield resin, immobilization of five nitrobenzoic acids was performed. Addition of four different alkenyl Grignard reagents and basic cleavage leads to substituted Me indolecarboxylates in excellent purities. Features of this reaction are the stability of halide groups, ester moieties, and tolerance of o,o’-unsubstituted nitro resins. Heck and Sonogashira reactions are also possible with immobilized indoles.

Organic Letters published new progress about Solid phase synthesis. 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, HPLC of Formula: 57663-18-0.

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

Lamotte, Yann published the artcileSynthesis and biological activities of novel indole derivatives as potent and selective PPARγ modulators, Synthetic Route of 57663-18-0, the main research area is biphenylcarboxylic acid indolylmethyl preparation peroxisome proliferator activated receptor modulator; acid biphenylcarboxylic indolylmethyl preparation PPAR gamma modulator potency SAR; indolylmethyl biphenylcarboxylic acid preparation antidiabetic PPAR partial agonist activity.

Starting from the structure of Telmisartan, a new series of potent and selective PPARγ modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds were reported and the X-ray structure of compound I bound to the PPARγ ligand binding domain was described.

Bioorganic & Medicinal Chemistry Letters published new progress about Hematocrit. 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Synthetic Route of 57663-18-0.

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

Ambrogio, Ilaria published the artcile3-(o-Trifluoroacetamidoaryl)-1-propargylic esters: common intermediates for the palladium-catalyzed synthesis of 2-aminomethyl-, 2-vinylic, and 2-alkylindoles, Name: Methyl 2-methyl-1H-indole-5-carboxylate, the main research area is amino methyl indole preparation; vinyl indole preparation; alkyl indole preparation.

3-(O-Trifluoroacetamidoaryl)-1-propargylic esters have been used as common synthetic intermediates for the preparation of a variety of 3-unsubstituted 2-substituted indoles. Treating Et 3-(o-trifluoroacetamidoaryl)-1-propargylic carbonates unsubstituted or containing an aryl substituent at the propargylic carbon with piperazines and Pd(PPh3)4 in THF at 80 °C affords 2-(piperazin-1-ylmethyl)indoles in excellent yields. Good to excellent yields of 2-aminomethylindoles are also obtained with other secondary amines. Et 3-(o-trifluoroacetamidoaryl)-1-propargylic carbonates bearing an alkyl substituent at the propargylic carbon and Et 3-(o-trifluoroacetamidoaryl)-1-propargylic acetates disubstituted at the propargylic carbon give 2-vinylic indoles with the Pd(OAc)2/PPh3 combination and Et3N in THF at 80 °C. Formation of 2-vinylic indoles is quite stereoselective, generating trans vinylic derivatives, at least with the substrates that we have investigated. In the presence of formic acid, Et3N, and Pd(PPh3)4 in MeCN at 80 °C, Et 3-(o-trifluoroacetamidoaryl)-1-propargylic carbonates afford 2-alkylindoles in good to excellent yields.

Tetrahedron published new progress about Heterocyclic compounds, nitrogen Role: SPN (Synthetic Preparation), PREP (Preparation). 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Name: Methyl 2-methyl-1H-indole-5-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

Soderberg, Bjorn C. G. published the artcileIntramolecular cyclization reactions of unsaturated amino Fischer chromium carbenes forming indoles and quinolines, Synthetic Route of 57663-18-0, the main research area is thermally induced intramol annulation alkenylphenylamino substituted Fischer chromium carbene; solvent effect intramol annulation alkenylphenylamino substituted Fischer chromium carbene; steric effect intramol annulation alkenylphenylamino substituted Fischer chromium carbene; inductive effect intramol annulation alkenylphenylamino substituted Fischer chromium carbene; electronic effect intramol annulation alkenylphenylamino substituted Fischer chromium carbene; aminostyrene intramol annulation alkenylphenylamino substituted Fischer chromium carbene; thermal decomposition intramol annulation alkenylphenylamino substituted Fischer chromium carbene; carbonyl alkylidene amino chromium Fischer carbene preparation intramol cyclization; amino carbonyl alkylidene chromium Fischer carbene preparation intramol cyclization; dubamine amino carbonyl alkylidene chromium Fischer carbene intramol cyclization; quinoline amino carbonyl alkylidene chromium Fischer carbene intramol cyclization; quinolinecarboxylic amino carbonyl alkylidene chromium Fischer carbene intramol cyclization; indole amino carbonyl alkylidene chromium Fischer carbene intramol cyclization; indolecarboxylic amino carbonyl alkylidene chromium Fischer carbene intramol cyclization.

A thermally induced intramol. annulation reaction of N-(2-alkenylphenyl)amino substituted Fischer chromium carbenes has been extensively examined The carbene complexes were prepared in moderate to good yields by reaction of 2-aminostyrenes with intermediately formed acyloxy substituted carbenes. Upon heating, the thermally labile carbenes decomposed producing indoles and quinolines as the major products. The product distribution was found to be highly dependent on the substitution pattern and electronic properties of the starting material, and on the solvent used. The reaction of pentacarbonyl[1-[[2-ethenyl-3-(methoxycarbonyl)phenyl]amino]ethylidene]chromium gave 2-methyl-1H-indole-4-carboxylic acid Me ester. The reaction of pentacarbonyl[1-[[2-(1-methylethenyl)phenyl]amino]ethylidene]chromium gave 2,4-dimethylquinoline and 1,2,3,4-tetrahydro-2,4-dimethylquinoline.

Tetrahedron published new progress about Cyclization. 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Synthetic Route of 57663-18-0.

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, Wen-Qian published the artcileDearomative Arylcyanation of Indoles via C-CN Bond Activation Enabled by Ni/Lewis Acid Cooperative Catalysis, Product Details of C11H11NO2, the main research area is isoindoloindole carbonitrile preparation stereoselective nickel Lewis acid cooperative catalysis; indolecarbonyl benzonitrile intramol dearomative arylcyanation.

A nickel/Lewis acid cooperatively catalyzed intramol. dearomative arylcyanation of indoles is presented. The reaction proceeds through a C-CN bond activation, dearomatization, and benzylic cyanation sequence, affording 3-cyano fused indolinyl heterocycles in good to excellent yields and excellent diastereoselectivity. The asym. version of the reaction can be established in moderate enantioselectivity by using a chiral ligand.

Organic Letters published new progress about Benzoyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Product Details of C11H11NO2.

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