| Alpha-aminoketones and their derivatives are widely present in drug molecules,bioactive molecules,and natural product molecules,such as the antidepressant bupropion,the platelet aggregation inhibitor prasugrel and clopidogrel,and the antitumor compound PRIMA-1.This structure is contained in both APR-246 and the natural product cathinone.At the same time,α-aminoketones are important organic synthesis intermediates and widely used in the synthesis of heterocyclic compounds.In view of the important role of α-aminoketones,their synthesis methods have long been widely studied.Among these synthetic methods,the simplest and most effective method is the direct oxidative amination of the ketone compound α-C(sp3)-H bond.However,these methods generally have disadvantages such as the need for transition metal catalysts and chemical oxidants.Therefore,the use of oxygen as an oxidant to achieve direct oxidative amination of ketones has important research significance without the participation of transition metals and chemical oxidants.In this paper,under the condition of no transition metal participation,use the oxygen in the air as the oxidant,and the oxidation and amination of various cyclic ketones are realized by using acid and alkali as the combined catalyst.The reaction not only suit for a wide range of substrates,but also provides a new method for the simple and efficient synthesis of α-amino enones and benzodiazepine derivatives.At the same time,it also provides a new way for the α-position of ketone compound functionalization.Since the method does not require a metal catalyst,only use oxygen in the air as an oxidant,which has the advantages of environmental protection,and thus has important significance and potential application value in organic synthesis. |
