A route to the direct amidation of aromatic-ring-tethered N-carbamoyl tetrahydroisoquinoline substrates was developed. This route enabled general access to 8-oxoberberines and their 5- and 7- membered C-ring homologues. It overcomes the undesired tandem side-reactions that result in the destruction of the isoquinoline backbone, which inevitably occurred under our previously reported superacidic carbamate
开发了直接酰胺化芳族环系N-
氨基甲酰基
四氢异喹啉底物的途径。该途径使人们能够普遍获得8-氧小ber碱及其5和7元C环同系物。它克服了导致
异喹啉主链破坏的不希望的串联副反应,这种副反应在我们先前报道的超酸性
氨基甲酸酯活化方法下不可避免地发生。