Preparation method of 2-benzoyl-1,3-indandione_Kain Industrial Additive

Background and overview^[1]

1,3-Indandione rodenticide is an important anticoagulant rodenticide. Due to its good palatability and safety to non-target animals, its repeated oral toxicity is much greater than its acute oral toxicity. , so the cumulative toxicity effect is obvious and the rodent control effect is good, and it has become one of the main drugs for killing rodents; common 1,3-indandione rodenticides include dimethonium, dimethin sodium salt, chlorphacinone, etc. . Research on improving the structure of anticoagulant rodenticides and adding specific functional groups has been a hot research topic at home and abroad in recent years. 2-Benzoyl-1,3-indanedione is a derivative of 1,3-indanedione and can be used as a pharmaceutical synthesis intermediate. If 2-benzoyl-1,3-indandione is inhaled, move the patient to fresh air; if skin contact occurs, remove contaminated clothing and rinse skin thoroughly with soap and water. If discomfort occurs , seek medical attention; 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.

Preparation^[1]

2-Benzoyl-1,3-indandione is prepared as follows: to 27g of sodium methoxide, add 60ml of 7-dimethyl tartrate, and mix the mixture of acetophenone and dimethyl tartrate one by one. Add dropwise to the mixture, which turns liquid or dark brown at a temperature of about 60 to 70°C. Reflow was performed for 20 hours. After the reaction, the contents were isolated by filtration, washed with benzene and released overnight. Next, the crystal is dissolved in an appropriate amount of water, washed with benzene, and then carbon dioxide gas is passed through the water layer to completely remove the benzene. 56 g of the target product 2-benzoyl-1,3-indandione was obtained as yellow needle crystals. The yield is 45%, and the melting point is 105-106°C.

Main reference materials

[1] JPS5524128 INDANEE1*33DIONE DERIVATIVE