RESUMO
Objective To investigate and optimize the syntheses of dimorpholine benzothiazole-phenylurea selective PI3Kβinhibitors. Methods With 2,4,6-three bromine aniline as the raw material,all the target compounds were prepared through thiophos?gene,cyclization,Buchwald-Hartwig cross coupling reaction and Suzuki coupling. The structures of intermediates and target com?pounds were characterized by MS and 1H NMR spectra. Results Six derivatives were synthesized. Compared with the method report?ed in the literature,the total yield of this new synthesis method increased from 16.2%to 26.9%. Conclusion The raw materials of op?timized 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.
RESUMO
The main compounds to treat HBV are nucleoside analogues and interferon,which generally possess the disadvan?tages of susceptibility to resistance,high cost and serious side effect. In order to overcome the problems above,a large amount of drugs are being developed,including the prodrug of nucleoside analogues(such as besifovir,CMX157 and tenofovir alafenamide),interfer?on(such as P1101)and antiviral drug based on certain new mechanisms(such as GS-9620,ARC520 and REP-9AC). Among them, the most attention is GS-9620 and REP-9AC,which could against HBV by strengthening body′s immune function. Immunotherapy has been a hot area of antiviral drug research nowadays. In this paper,we review the recent research of a series of new anti-HBV drugs which are undergoing clinical phases.