| 摘要 |
The present invention discloses a method of synthesizing an α-amino acid derivative with α-alkyl side chain substitution. The method comprises: reacting an alkene with 9-bbn at 0-80˚C for 0.5-12 h, and then adding an imine to react at 0-90˚C for 12-48 h with the presence of a transition metal salt, a base and an organic solvent to generate an α-amino acid derivative. In the present invention, an alkene is employed to in-situ generate an alkyl boron reagent, wherein the reaction condition is mild and the alkaline can be selected from a wide range. For the existing synthesis methods, a strict anhydrous and anaerobic condition is required, complex reaction operations are involved, and a low temperate is needed for the reaction to occur, thus causing a high cooling cost. On the contrary, the present invention does not require an anhydrous and anaerobic condition, and the reaction can occur at the room temperature or a slightly higher temperature. |
