199800-49-2

Usage

Uses

Used in Pharmaceutical Industry:
AG-041R is used as a therapeutic agent for the treatment of conditions related to the overactivation of the CCKB receptor. Its selective binding to the CCKB receptor helps in modulating the effects of cholecystokinin, a hormone that plays a role in various physiological processes, including digestion and the regulation of satiety.
Used in Research and Development:
In the field of research, AG-041R is utilized as a research tool to study the role of CCKB receptors in various biological processes and diseases. Its selective binding property allows scientists to investigate the specific functions and interactions of the CCKB receptor, leading to a better understanding of its role in the body and the development of targeted therapies.
Used in Cancer Treatment:
AG-041R has been found to have potential applications in cancer treatment, particularly in the context of tumors that overexpress CCKB receptors. By blocking the CCKB receptor, AG-041R may help in inhibiting tumor growth and progression, making it a promising candidate for the development of targeted cancer therapies.
Used in Gastrointestinal Disorders:
AG-041R is used as a treatment option for gastrointestinal disorders that involve the overactivation of the CCKB receptor, such as irritable bowel syndrome (IBS) and gastroesophageal reflux disease (GERD). By selectively blocking the CCKB receptor, AG-041R can help in reducing the symptoms associated with these conditions and improve the quality of life for patients.

InChI:InChI=1/C31H36N4O5/c1-5-39-28(40-6-2)20-35-26-10-8-7-9-25(26)31(29(35)37,19-27(36)32-23-15-11-21(3)12-16-23)34-30(38)33-24-17-13-22(4)14-18-24/h7-18,28H,5-6,19-20H2,1-4H3,(H,32,36)(H2,33,34,38)/t31-/m1/s1

Upstream product

• 159884-50-1 [1-(2,2-diethoxy-ethyl)-2-oxo-3-(3-p-tolyl-ureido)-2,3-dihydro-1H-indol-3-yl]-acetic acid 
• 106-49-0 p-toluidine 
• 159884-54-5 1-(2,2-diethoxyethyl)-1H-indole-2,3-dione 3-(O-methyloxime) 
• 195451-17-3 N-[1-(2,2-diethoxyethyl)-2,3-dihydro-2-oxo-1H-indol-3-yl]-N'-(4-methylphenyl)urea 
• 159883-92-8 [(R)-1-(2,2-diethoxyethyl)-2-oxo-3-(3-p-tolylureido)-2,3-dihydro-1H-indol-3-yl]acetic acid (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl ester 
• 91-56-5 indole-2,3-dione 
• 107976-78-3 1H-indole-2,3-dione 3-(O-methyloxime) 
• 1188395-65-4 (R)-1-(2,2-diethoxyethyl)-1′-(p-tolyl)-1′H-spiro[indoline-3,4′-pyrimidine]-2,2′,6′(3′H,5′H)-trione 
• 159884-41-0 1-(2,2-diethoxyethyl)indoline-2,3-dione 
• 1188395-64-3 (R)-methyl 2-(2-oxo-3-(3-p-tolylureido)indolin-3-yl)acetate 
• 1207340-46-2 (R)-(3-amino-2-oxo-2,3-dihydro-1H-indol-3-yl)-acetic acid methyl ester 
• 5343-65-7 2-bromo-N-p-tolylacetamide 

Relevant academic research and scientific papers

Catalytic Enantioselective Decarboxylative Mannich-Type Reaction of N-Unprotected Isatin-Derived Ketimines

The first catalytic enantioselective decarboxylative Mannich-type reaction of N-unprotected ketimines is reported, directly providing N-unprotected 3-tetrasubstituted 3-aminooxindoles in high yield and ee without protection/deprotection steps. The utility

A process for preparing AG - 041 R new method (by machine translation)

The invention discloses a method for preparing AG - 041 R of the new method, it mainly comprises the following steps: the R - 2 - (3 - amino - 2 - oxo indole - 3 - yl) acetic acid methyl ester with the 1st 1st alkaline substance is placed in the solvent, addition of amino protective agent, to obtain the intermediate V; the intermediate V, 2nd alkaline material, bromine acetaldehyde diethyl acetal is placed in 2nd solvent, stirring the reaction, to obtain the intermediate IV; the intermediate IV, methyl aniline and 3rd 3rd alkaline substance is placed in the solvent, stirring under ice bath carries out amidation reaction, to obtain the intermediate III; the intermediate III with the catalyst is placed 4th in the solvent, the reaction of the hydrogen gas, filtering to remove the catalyst, to obtain the intermediate II; the intermediate II with the toluene isocyanate is placed in the 5th solvent, stirring at room temperature the reaction, the target product. The present invention provides a process for preparing AG - 041 R of the new method, it has simple process operation, high yield, low cost, product purity and the like, and is suitable for industrial production. (by machine translation)

An asymmetric acetate-Mannich reaction of chiral isatin derived ketimines and its applications

A highly efficient TMSOTf-mediated asymmetric acetate-Mannich reaction of isatin derived tert-butylsulfinyl ketimines and S-phenyl thioacetate was developed to afford the direct synthesis of indole-based β3,3-amino acid thioester with excellent selectivity (dr > 98 : 2). Syntheses of (+)-AG-041R and 3-aminopyrroloindoline have been accomplished utilizing the developed method.

Resorcinarene sulfonylated cinchona alkaloid amine compd. heterointerface

PROBLEM TO BE SOLVED: To provide a heteroarenesulfonyl cinchona alkaloid amine catalyst which solves the problems about the lowness of steric selectivity/reactivity of each product even if any of many asymmetric organic molecular catalysts used for the control of asymmetric space are used.SOLUTION: The heteroarenesulfonyl cinchona alkaloid amine compound catalyst is obtained by introducing a hetroarylsulfonyl group onto the nitrogen atom of cinchona alkaloid to form an intramolecular hydrogen bond between the amide hydrogen of the sulfonamide and the hetero atom. A method for manufacturing a β-aminocarbonyl compound using the same is also provided.

Enantioselective synthesis of AG-041R by using N-heteroarenesulfonyl cinchona alkaloid amides as organocatalysts

The organocatalytic enantioselective decarboxylative addition of malonic acid half thioesters to ketimines derived from isatins by using N-heteroarenesulfonyl cinchona alkaloid amides afforded products with high enantioselectivity. The products could be c

An expedient route to a potent gastrin/CCK-B receptor antagonist (+)-AG-041R

(Chemical Equation Presented) An enantiocontrolled synthesis of (+)-AG-041R (1), a potent gastrin/CCK-B receptor antagonist, has been achieved employing a chiral rhodium(II)-catalyzed, oxidative intramolecular aza-spiroannulation as the key step. 2009 Ame

Highly enantioselective intramolecular aza-spiroannulation onto indoles using chiral rhodium catalysis: Asymmetric entry to the spiro-β-lactam core of chartellines

A versatile, highly enantiocontrolled entry to the spiro-β-lactam core of chartellines has been developed by expanding the scope of oxidative nitrogen atom transfer methodology based on chiral Rh-nitrenoid species.

Efficient asymmetric synthesis of novel gastrin receptor antagonist AG-041R via highly stereoselective alkylation of oxindole enolates

An efficient method for asymmetric synthesis of the potent Gastrin/CCK-B receptor antagonist AG-041R was developed. Core oxindole stereochemistry was established by asymmetric alkylation of oxindole enolates with bromoacetic acid esters, using l-menthol a