Bharate Jaideep B, Abbat Sheenu, Sharma Rohit, Bharatam Prasad V, Vishwakarma Ram A, Bharate Sandip B
Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu-180001, India.
Org Biomol Chem. 2015 May 14;13(18):5235-42. doi: 10.1039/c5ob00419e.
A cobalt acetylacetonate catalyzed oxidative diketonation of alkynes via C(sp)-H bond functionalization has been described. The reaction involves a free-radical mechanism, wherein the phenyl radical formed from phenyl hydrazine couples with Co(II) activated alkyne to produce 1,2-diketones. The reaction proceeds at room temperature in DMF with the use of Ag2O/air as the oxidizing system. The utility of the protocol for the synthesis of a series of imidazoles including a potent platelet aggregation inhibitor trifenagrel has been demonstrated.
已报道了一种乙酰丙酮钴催化的通过C(sp)-H键官能团化实现炔烃氧化二酮化反应。该反应涉及自由基机理，其中由苯肼形成的苯基自由基与钴（II）活化的炔烃偶联生成1,2-二酮。该反应在室温下于N,N-二甲基甲酰胺中进行，使用氧化银/空气作为氧化体系。已证明该方法在合成一系列咪唑类化合物（包括强效血小板聚集抑制剂三氟醋柳酯）中的实用性。
