Key Laboratory of Organo-Pharmaceutical Chemistry of Jiangxi Province, Gannan Normal University, Ganzhou 341000, China.
J Org Chem. 2022 May 6;87(9):6224-6236. doi: 10.1021/acs.joc.2c00452. Epub 2022 Apr 20.
An efficient copper-catalyzed aerobic oxidative cross-dehydrogenative coupling reaction for the synthesis of multisubstituted phosphorylhydrazides from ,-disubstituted hydrazines and hydrogen phosphoryl compounds is accomplished. The reaction proceeds under mild conditions without the addition of any external oxidants and bases. This work reported here represents a direct P(═O)-N-N bond formation with the advantages of being operationally simple, good functional group tolerance, and high atom and step economy. Furthermore, the selected compounds exhibit potential inhibitory activity against tumor cells, which can be used in the field of screening of anticancer agents as new chemical entities.
一种高效的铜催化有氧氧化交叉脱氢偶联反应，用于从，-二取代腙和氢膦化合物合成多取代的磷酰基腙。该反应在温和的条件下进行，无需添加任何外部氧化剂和碱。这里报道的这项工作代表了直接的 P(=O)-N-N 键形成，具有操作简单、良好的官能团耐受性和高原子经济性和步骤经济性的优点。此外，所选化合物对肿瘤细胞表现出潜在的抑制活性，可作为新的化学实体用于抗癌药物的筛选领域。
