A Practical Synthesis of Regioisomeric 6-and 7-Methoxytetrahydro-3-benzazepines

被引:6
作者
Liang, Jimmy T. [1 ]
Liu, Jing [1 ]
Shireman, Brock T. [1 ]
Tran, Vi [1 ]
Deng, Xiaohu [1 ]
Mani, Neelakandha S. [1 ]
机构
[1] Johnson & Johnson Pharmaceut Res & Dev LLC, San Diego, CA 92121 USA
关键词
DOPAMINE D-1 ANTAGONIST; FUSED BENZAZEPINE; STEREOSELECTIVE SYNTHESES; BIOLOGICAL EVALUATION; RECEPTOR ANTAGONISTS; SCH; 39166; POTENT; SERIES;
D O I
10.1021/op900292j
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
A concise and versatile synthetic route for 6- and 7-methoxy tetrahydro-3-benzazepines is described. The key feature of the synthesis is a one-pot acylatioti/cyclizaition/elimination sequence to construct either of the isomeric dihydrobenzazepine ring systems from the same starting material. The route is high yielding and chromatography-free.
引用
收藏
页码:380 / 385
页数:6
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