| 摘要 |
The present invention relates to a sequential method for converting a substrate with general formula (5), where X = O or NH, R = alkyl or aryl and n = 0 or 1, into a product with general formula (6), where R2 = alkyl, alyl, aryl or heteroaryl, and R3 = H, alkyl; or R2 and R3 can be connected forming a cycle, characterised in that said method includes the steps of: [a] radical decarboxylation of the substrate (5); [b] oxidation of the intermediate formed in step [a] to produce an intermediate (7); and [c] stereoselective addition of a nucleophile to the acyliminium ion (7) formed in step [b]; obtaining products (6) having high optical purity. (F). The present invention also relates to the use of the described method for preparing libraries of novel derivatives of the compounds with formula (6), which could be used as such or derivatised in order to obtain bioactive products such as alkaloids or imino sugars, or to obtain chiral ligands. |
