background and overview[1]
dimethyl 2-aminoisophthalate can be used as an intermediate for pharmaceutical and chemical synthesis. if 2-aminoisophthalate dimethyl ester is inhaled, move the patient to fresh air; if skin contact occurs, take off contaminated clothing, rinse the skin thoroughly with soap and water, and seek medical attention if you feel uncomfortable; if eye contact occurs, separate eyelids, rinse with running water or saline, and seek medical attention immediately; if ingested, rinse mouth immediately, do not induce vomiting, and seek medical attention immediately.
apply[1]
2-aminoisophthalic acid dimethyl ester can be used as a pharmaceutical and chemical synthesis intermediate. for example, it can be used to prepare 2-(methylsulfonylamino)isophthalic acid dimethyl ester. the specific steps are: methylsilyldiazamethane (9.12 ml, 18.24 mmol) (2m in diethyl ether) was slowly added to 9 ml of anhydrous 2-amino-3-(methoxycarbonyl)benzoic acid (2.0 g, 10.25 mmol). a solution of tetrahydrofuran and 6 ml of methanol was then stirred at room temperature overnight. the reaction mixture was concentrated and purified by flash chromatography (1-6% methanol/ch2cl2) to give the intermediate. then a mixture of the above compound (1.50g, 7.17mmol), pyridine (1.74ml, 21.51mmol) and methanesulfonic anhydride (2.50g, 14.34mmol) in 60ml 1,2-dichloroethane was stirred at 80°c overnight. . the reaction mixture was concentrated and the residue was purified by flash chromatography (0-7% methanol/chcl) to give the title compound 2-(methylsulfonylamino)isophthalic acid dimethyl ester.
preparation [1]
dimethyl 2-aminoisophthalate was prepared as follows: trimethylsilyldiazamethane (9.12 ml, 18.24 mmol) (2m in ether) was slowly added to 2-amino-3 – (methoxycarbonyl)benzoic acid (2.0 g, 10.25 mmol) was dissolved in anhydrous 9 ml of tetrahydrofuran and 6 ml of methanol, and the mixture was stirred at room temperature overnight. the reaction mixture was concentrated and purified by flash chromatography (1-6% methanol/ch2cl2) to give the title compound 2-aminoisophthalic acid dimethyl ester.
main reference materials
[1] us20130018045. chemical entities to be used for wee1 inhibition for the treatment of cancer