214288-97-8Relevant academic research and scientific papers
Eco-efficient one-pot synthesis of quinazoline-2,4(1H,3H)-diones at room temperature in water
Tian, Xin-Chuan,Huang, Xing,Wang, Dan,Gao, Feng
, p. 824 - 829 (2016/10/06)
An efficient one-pot synthesis of quinazoline-2,4(1H,3H)-diones was developed. First, the reactions of anthranilic acid derivatives with potassium cyanate afforded the corresponding urea derivatives. Then, cyclization of the urea derivatives with NaOH afforded the monosodium salts of benzoylene urea. Finally, HCl treatment afforded the desired products in near-quantitative yields. This is an eco-efficient method because all the reactions were carried out in water, and the desired products were obtained simply by filtration. The aqueous filtrate was the only waste generated from the reaction. We scaled up the reaction to 1 kg starting material, thus establishing an alternative approach for the green synthesis of quinazoline-2,4(1H,3H)-diones in the chemical and pharmaceutical industries.
The process development of a novel aldose reductase inhibitor, FK366. Part 1. Improvement of discovery process and new syntheses of 1-substituted quinazolinediones
Goto, Shunsuke,Tsuboi, Hiroyuki,Kanoda, Masami,Mukai, Koji,Kagara, Kooji
, p. 700 - 706 (2013/09/05)
This contribution describes part 1 of process development of a novel aldose reductase inhibitor FK366 (1). The original process applied on a laboratory scale was improved from the safety viewpoint to manufacture materials on 500-L scale suitable for toxic
