Syntheses of dimorpholine benzothiazole-phenylurea selective PI3Kß inhibitors / 国际药学研究杂志

ABSTRACT

Objective To investigate and optimize the syntheses of dimorpholine benzothiazole-phenylurea selective PI3Kß inhibitors. Methods With 2, 4, 6-three bromine aniline as the raw material, all the target compounds were prepared through thiophosgene, cyclization, Buchwald-Hartwig cross coupling reaction and Suzuki coupling. The structures of intermediates and target compounds were characterized by MS and 1H NMR spectra. Results Six derivatives were synthesized. Compared with the method reported in the literature, the total yield of this new synthesis method increased from 16.2% to 26.9%. Conclusion The raw materials of optimized synthesis method are cheap and easy to obtain, and the reaction operation steps are simplified. The post-processing process avoids steps of column chromatography and improves the experimental efficiency.