Concise Synthesis of 2-Benzazepine Derivatives and Their Biological Activity
Concise Synthesis of 2-Benzazepine Derivatives and Their Biological Activity
复制标题
DOI：
10.1021/jo300380z
复制
发表时间：
2012-04-20
影响因子：
3.6
通讯作者：
Kamimura, Akio
中科院分区：
文献类型：
--
作者：
So, Masahiro;Kotake, Tomoko;Kamimura, Akio
2-苯并氮杂平是治疗皮肤伤口的新药物疗法的潜在良好候选者，可以通过分子内弗里德尔克拉夫茨反应很容易地由取代的肉桂酰胺制备。该方法只需少量步骤和有效反应，即可快速衍生化 2-苯并氮杂卓类药物。此外，光学活性的4-取代-2-苯并氮杂是由手性α-取代的肉桂酰胺制备的，其可以通过手性肉桂基恶唑烷酮酰胺的不对称α-烷基化容易地制备。我们轻松地制备了 20 多种衍生物的库，并检查了这些化合物的生物活性。
2-Benzazepines, which are potentially good candidates for new drug therapies to treat skin wounds, were readily prepared from substituted cinnamylamide via an intramolecular Friedel Crafts reaction. With few steps and effective reactions, the procedure enables a rapid derivatization of 2-benzazepines. Moreover, optically active 4-substituted-2-benzazepines were prepared from chiral alpha-substituted cinnamylamides, which were readily prepared by asymmetric alpha-alkylation of chiral cinnamyl oxazolidinone amides. We have easily prepared a library of more than 20 derivatives and examined the biological activity of the compounds.