| 发明名称 | 6-piperazinyl-3,4-dihydroquinazolin-2(1<i>H</i>)-ones | ||
| 摘要 | A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds. | ||
| 申请公布号 | US9145388(B2) | 申请公布日期 | 2015.09.29 |
| 申请号 | US201414184339 | 申请日期 | 2014.02.19 |
| 申请人 | King Fahd University of Petroleum and Minerals;King Abdulaziz City for Science Technology | 发明人 | Ullah Nisar |
| 分类号 | A61K31/517;C07D401/12;C07D239/80 | 主分类号 | A61K31/517 |
| 代理机构 | Oblon, McClelland, Maier & Neustadt, L.L.P. | 代理人 | Oblon, McClelland, Maier & Neustadt, L.L.P. |
| 主权项 | 1. A dihydroquinolinone compound of formula (1) wherein R is selected from the group consisting of: | ||
| 地址 | Dhahran SA | ||