810696-50-5

Upstream product

• 2840-02-0 5-acetamido-2-bromobenzoic acid 
• 6942-37-6 5-amino-2-bromo-benzoic acid methyl ester 
• 600-00-0 ethyl 2-bromoisobutyrate 
• 810696-49-2 methyl 3-amino-6-bromo-2-nitrobenzoate 

Relevant academic research and scientific papers

Production method for 3, 3-dimethyl-3, 4-dihydro-1h-quinoxaline-2-one derivative and intermediate for said production method

To provide: a novel production method suitable for industrial production of a 3, 3-dimethyl-3, 4-dihydro-1H-quinoxaline-2-one derivative; and a synthetic intermediate therefor. Provided is a production method is for a compound indicated by formula (1) or a salt thereof, said production method including: a step in which a compound indicated by formula (2) or a salt thereof is reacted with a nitrating agent and a compound indicated by formula (3) or a salt thereof is obtained; and a step in which the compound indicated by formula (3) or a salt thereof is reduced and a compound indicated by formula (1) or a salt thereof is obtained. (Each symbol in the formulas (1, 2, 3) is the same as in the definitions in claim 1.)

PRODUCTION METHOD FOR 3,3-DIMETHYL-3,4-DIHYDRO-1H-QUINOXALIN-2-ONE DERIVATIVE AND INTERMEDIATE FOR SAID PRODUCTION METHOD

An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method. Provided is a method for producing a compound represented by formula (1): wherein R1 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, R2 represents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or nitrogen atom-protecting group, R3 represents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or a nitrogen atom-protecting group, and X represents a hydroxy group or a leaving group, or a salt thereof, the method comprising the steps of: reacting a compound represented by formula (2): wherein R1, R2, and X are the same as defined in formula (1), R4 represents an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, or a salt thereof with a nitrating agent to obtain a compound represented by formula (3) wherein R1, R2, R4, and X are the same as defined in formulae (1) and (2), or a salt thereof, and reducing the compound represented by formula (3) or the salt thereof to obtain the compound represented by formula (1) or the salt thereof.

Development of a practical synthesis of 7-bromo-8-methoxycarbonyl-3,3-dimethyl-3,4-dihydro-1hquinoxalin- 2-one

Synthesis of 7-bromo-8-methoxycarbonyl-3,3-dimethyl-3,4-dihydro- 1H-quinoxalin-2-one from 5-amino-2-bromobenzoic acid was achieved in an overall yield of 27% over four steps. This is a significant improvement from the previous six-step process, which affo

NOVEL 1,2,3,4-TETRAHYDROQUINOXALINE DERIVATIVE HAVING GLUCOCORTICOID RECEPTOR BINDING ACTIVITY

An object of the present invention is to synthesize a novel 1,2,3,4-tetrahydroquinoxaline derivative represented by formula (1) and to find a pharmacological action of the derivative. In the formula, the R1 represents a halogen, an alkyl, cycloalkyl, aryl or heterocyclic group, or the like; p represents 0 to 5; R2 represents a halogen, an alkyl, hydroxyl or alkoxy group, or the like; q represents 0 to 2; R3 represents hydrogen, an alkyl, alkenyl, alkylcarbonyl or arylcarbonyl group, or the like; R4 and R5 independently represent hydrogen, a halogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; R6 represents hydrogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; and X represents O or S.