School of Pharmacy , Guizhou Medical University , Guiyang 550004 , China.
State Key Laboratory of Functions and Applications of Medicinal Plants , Guizhou Medical University , Guiyang 550014 , China.
J Org Chem. 2018 Mar 16;83(6):3348-3353. doi: 10.1021/acs.joc.7b02961. Epub 2018 Feb 23.
The palladium-catalyzed cross-coupling reaction of aryl halides with isoquinoline-1,3(2 H,4 H)-diones for the synthesis of 4-aryl isoquinoline-1,3(2 H,4 H)-diones was developed. The reaction conditions exhibit remarkable compatibility with various aryl halides and isoquinoline-1,3(2 H,4 H)-diones, and the product could be conveniently transformed to 4-aryl tetrahydroisoquinolines. (±) Dichlorofensine was synthesized using this protocol in two steps with an overall yield of 71%.
发展了钯催化的芳基卤化物与异喹啉-1,3(2H,4H)-二酮的交叉偶联反应，用于合成 4-芳基异喹啉-1,3(2H,4H)-二酮。该反应条件与各种芳基卤化物和异喹啉-1,3(2H,4H)-二酮具有显著的相容性，产物可以方便地转化为 4-芳基四氢异喹啉。（±）二氯芬辛通过该方案两步合成，总收率为 71%。
