870459-83-9

Upstream product

• 769-92-6 4-tert-Butylaniline 
• 105-36-2 ethyl bromoacetate 
• 623-73-4 diazoacetic acid ethyl ester 

Downstream Products

• 911846-66-7 1-(4-tert-butyl-phenyl)-6-chloro-3-(4-trifluoromethyl-pyridin-2-yloxy)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid ethyl ester 
• 911842-12-1 1-(4-tert-butyl-phenyl)-6-methoxy-3-(3-trifluoromethyl-phenoxy)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid ethyl ester 
• 911843-18-0 1-(4-tert-butyl-phenyl)-6-chloro-3-(3-trifluoromethyl-phenoxy)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Ethyl cellulose derived porous iron@N-doped carbon material for N–H carbene insertion reaction

A newly developed, facile and sustainable strategy, in which zinc salt, melamine and ethyl cellulose are applied as pore-forming agent, nitrogen and carbon source respectively, has been disclosed for the synthesis of Fe/N-codoped carbon materials. This material exhibits excellent catalytic efficiency towards N–H carbene insertion reaction for the synthesis of unnatural amino acid derivatives. Fe/FeOx nanoparticles tranfer electrons to N-doped carbon owing to the Mott-Schottky Effect, which is beneficial to the formation of iron carbene intermediate. N-doping can offer more Lewis base sites, which promotes the proton transfer process. Fe/FeOx nanoparticles are coated with graphitic carbon, thereby avoiding the loss and deactivation of iron sites in this material. Therefore, this material can be reused at least four times without significant loss in activity.

Molecular Oxygen-Mediated Radical Alkylation of C(sp3)-H Bonds with Boronic Acids

A direct and site-specific alkylation of (sp3)C-H bond with aliphatic boronic acid was achieved. By simply heating glycinates and amines together with alkylboronic acids under an oxygen atmosphere, a variety of unnatural α-amino acids and peptides could b

Preparation method of N-aryl glycine ester derivative

The invention relates to a preparation method of an N-aryl glycine ester derivative. The invention aims to solve the problems of complex steps and environmental pollution in the existing method for synthesizing the N-aryl glycine ester derivative. The preparation method comprises the following steps: dissolving an aryl primary amine compound, ethyl diazoacetate, a reaction aid and a photocatalystin an organic solvent at room temperature, uniformly mixing, reacting under a blue LEDs lamp, carrying out reduced pressure distillation to remove the solvent, and separating and purifying to obtain the product. The problems of high energy consumption, high cost and environmental pollution caused by high temperature, biocatalyst or metal organic framework required by the synthesis of the existingN-aryl glycine ester derivative are solved. A route for synthesizing the N-arylglycine ester derivative, which is green, efficient, mild in condition, simple in method, convenient to operate and highin yield, is found, and the method is applied to the field of organic synthesis.

Unnatural α-Amino Acid Synthesized through α-Alkylation of Glycine Derivatives by Diacyl Peroxides

We have developed a protocol for catalyst- and additive-free α-alkylation reactions of glycine derivatives with diacyl peroxides, which proceed by a pathway involving addition of alkyl radicals to imine intermediates. The diacyl peroxide substrate acts as both alkylation agent and oxidizing agent, which means it is atom-economical. It was applied to various glycine derivatives, dipeptides, and a 3,4-dihydroquinoxalin-2(1H)-one derivative and could be carried out on a gram scale, indicating its utility for late-stage functionalization.

Copper catalysis: One-pot simultaneous synthesis of quinolines and gem-diamine derivatives

A copper(II)-catalyzed oxidative reaction for the one-pot simultaneous synthesis of quinolines and gem-diamine derivatives from N-arylglycine ethyl esters and enamides is described. In this reaction, the two fragments in an enamide substrate react with th

FERROCHELATASE INHIBITORS AND METHODS OF USE

The invention relates to a method of treatment of a patient with a ferrochelatase inhibitor, or a pharmaceutically acceptable salt thereof, or a derivative thereof. Also, the invention relates to a method of treatment of a patient with a ferrochelatase in

MYOGLOBIN-BASED CATALYSTS FOR CARBENE TRANSFER REACTIONS

Methods are provided for carrying out carbene transfer transformations such as olefin cyclopropanation reactions, carbene heteroatom-H insertion reactions (heteroatom = N, S, Si), sigmatropic rearrangement reactions, and aldehyde olefination reactions with high efficiency and selectivity by using a novel class of myoglobin-based biocatalysts. These methods are useful for the synthesis of a variety of organic compounds which contain one or more new carbon-carbon or carbon-heteroatom (N, S, or Si) bond. The methods can be applied for conducting these transformations in vitro (i.e., using the biocatalyst in isolated form) and in vivo (i.e., using the biocatalyst in a whole cell system).

Myoglobin-catalyzed intermolecular carbene N-H insertion with arylamine substrates

Engineered variants of the heme-containing protein myoglobin can efficiently catalyze the insertion of α-diazo esters into the N-H bond of arylamines, featuring a combination of high chemoselectivity, elevated turnover numbers, and broad substrate scope.

Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARγ partial agonists

A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARγ modulators. Their chemical synthesis and in vitro activities are discussed. Compound 5 was selected for in vivo testing in the db/db mouse model of type 2 diabetes and resulted in reduction of hyperglycemia at comparable plasma exposure when compared to rosiglitazone.