1141475-82-2

Upstream product

• 13531-48-1 methyl 3-cyanobenzoate 
• 1877-72-1 3-Cyanobenzoic acid 

Downstream Products

• 15676-11-6 3-(carbamimidoyl)benzoic acid methyl ester 
• 775304-57-9 ataluren 
• 775304-60-4 3-((5-(2-fluorophenyl))-(1,2,4-oxadiazol-3-yl))benzoic acid methyl ester 
• 775304-80-8 3-(N-2-fluorobenzoylcarbamimidoyl)-benzoic acid methyl ester 
• 1072438-67-5 3-[5-(3-cyano-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid methyl ester 
• 1609643-66-4 methyl 3-(5-(2,4-dichlorophenyl)-1,2,4-oxadiazol-3-yl)benzoate 
• 912461-75-7 3-(N-2-fluorobenzoylamidino)benzoic acid methyl ester 

Relevant academic research and scientific papers

Preparation method of Ataluren

The invention discloses a preparation method of Ataluren. The preparation method comprises an addition step in which under an alkaline condition, 3-cyanobenzoate reacts with hydroxylamine hydrochloride by using a first mixed solvent to obtain an intermediate as shown in a formula III, a condensation step in which in a first organic solvent, a condensation reaction is conducted on the intermediate shown in the formula III and o-fluorobenzoic acid to obtain an intermediate shown in a formula IV, a cyclization step in which in a second organic solvent, catalyzing is conducted by using Lewis acid, and intramolecular dehydration is conducted on the intermediate in the formula IV to obtain an intermediate in a formula V, and an ester hydrolysis step in which under an alkaline condition, ester hydrolysis is conducted on the intermediate in the formula V by using a second mixed solvent to obtain the product. Cheap raw materials are subjected to addition, condensation, cyclization and ester hydrolysis, the reaction conditions are mild, the process is simple, the cost is low, and industrial production is facilitated. Meanwhile, the solvent in the reaction process can be basically recycled, the synthesis cost is low, and the reaction environment is good; in addition, the purification operation is simple, and the total yield and the product purity of the target compound Ataluren are high.

Pyrazol-1, 2, 4-oxadiazole substituted benzamide compound as well as preparation method and application of pyrazol-1, 2, 4-oxadiazole substituted benzamide compound

The invention belongs to the technical field of chemical synthesis and medicine application, and particularly relates to a pyrazol-1, 2, 4-oxadiazole substituted benzamide compound as well as a preparation method and application of the pyrazol-1, 2, 4-oxadiazole substituted benzamide compound. The preparation method comprises the following steps: reacting methyl 3-cyanobenzoate with hydroxylamine hydrochloride to obtain an intermediate 3, then carrying out ring synthesis on the intermediate 3 and pyrazole acid to obtain pyrazol-1, 2, 4-oxadiazole substituted methyl benzoate, and finally carrying out hydrolysis and condensation to obtain the pyrazol-1, 2, 4-oxadiazole substituted benzamide compound. According to the present invention, the structure of the obtained product is confirmed through the nuclear magnetic hydrogen spectrum, the bactericidal activity test is performed on the obtained 18 target products, and the results show that the target product obtained through the preparation method has good antibacterial activity at the concentration of 50 ppm, and the inhibition rate on the rhizoctonia solani within 7 h can achieve 100%.

Method for preparing ataluren

The invention discloses a method for preparing ataluren, (PTC124, a commodity name of ataluren) and belongs to the field of organic synthesis. The preparation method comprises the following steps: (1)reacting methyl m-cyanobenzoate with hydroxylamine hydrochloride in a lower alcohol or a mixed solvent of a lower alcohol and water to generate 3-(N-hydroxyamidino)-methyl benzoate; (2) carrying outO-acylation reaction between the 3-(N-hydroxyamidino)-methyl benzoate and o-fluorobenzoyl chloride in an organic solvent to obtain 3-((5-(2-fluorophenyl))-3-(1,2,4-oxadiazolyl)-methyl benzoate; (3) under the catalytic action of tetra-alkyl ammonium halide, carrying out cyclization to obtain 3-((5-(2-fluorophenyl))-3-(1,2,4-oxadiazolyl)-methyl benzoate; and (4) hydrolyzing to obtain ataluren. The synthesis method is a simple and efficient synthesis method of ataluren.

KCNT1 INHIBITORS AND METHODS OF USE

The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.

Palladium-Catalyzed, Silver-Assisted Direct C-5–H Arylation of 3-Substituted 1,2,4-Oxadiazoles under Microwave Irradiation

A direct C-5–H arylation of 3-substituted 1,2,4-oxadiazoles with aryl iodides in the presence of a palladium catalyst and silver acetate is reported. This method provides a rapid, reliable way to obtain versatile 3,5-diaryl-1,2,4-oxadiazole derivatives, which are common moieties of many biologically active molecules. The synthetic applications of this novel method have been demonstrated in the concise syntheses of Ataluren and a potent RET inhibitor Yhhu251. (Figure presented.).

NOVEL TRIAZINE COMPOUND, ULTRAVIOLET ABSORBER AND RESIN COMPOSITION USING THE SAME

PROBLEM TO BE SOLVED: To provide a triazine compound useful as an ultraviolet absorber in fields of a polymeric material, a coating, a fiber, a surface coating material, a cosmetic raw material and a photography material or the like. SOLUTION: There is provided the compound represented by the general formula (I). (I), where R represents an alkyl group, an aryl group, a hydroxyl group, an alkoxy group, an aryloxy group, a heterocyclic oxy group, an alkylcarbonyloxy group, an arylcarbonyloxy group, a carbamoyloxy group, a formyl group, a carboxyl group, an alkylcarbonyl group, an arylcarbonyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, a cyano group, a nitro group, an amino group, an ureido group, a carbamoyl group, a sulfamoyl group, a sulfonic group, an alkylthio group, an arylthio group, a heterocyclic thio group, an alkylsulfonyl group, arylsulfonyl group, a heterocyclic residue or a halogen atom. These substituents may further be substituted. COPYRIGHT: (C)2016,JPO&INPIT

ANTIVIRAL COMPOUNDS AND USE THEREOF

The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.

TRIAZOLE OXADIAZOLES DERIVATIVES

The invention relates to compounds of formula (I), wherein R1, R2, Ra, Rb, X have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

METHODS FOR DOSING AN ORALLY ACTIVE 1,2,4-OXADIAZOLE FOR NONSENSE MUTATION SUPPRESSION THERAPY

The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.

METHODS FOR THE PRODUCTION OF FUNCTIONAL PROTEIN FROM DNA HAVING A NONSENSE MUTATION AND THE TREATMENT OF DISORDERS ASSOCIATED THEREWITH

The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.