Bell Christan E, Shaw Arthur Y, De Moliner Fabio, Hulme Christopher
Department of Chemistry and Biochemistry, The University of Arizona, Tucson, AZ 85721.
College of Pharmacy, Department of Pharmacology and Toxicology, BIO5 Oro Valley, 1580 E. Hanley Blvd., The University of Arizona, Oro Valley, AZ 85737.
Tetrahedron. 2014 Jan 7;7(1):54-59. doi: 10.1016/j.tet.2013.11.035.
A tunable microwave-assisted protocol for the synthesis of two biologically relevant families of heterocycles has been designed. Via a simple switch of reaction conditions, the same starting materials can be engaged in either an improved synthesis of the dihydrotriazine scaffold or a novel, first-in-class MCR to render the challenging 5-aminoimidazole nucleus in a single step. An additional first in class MCR is also reported utilizing guanidines to afford 2,5-aminoimidazoles.
设计了一种用于合成两类具有生物学相关性杂环化合物的可调谐微波辅助方案。通过简单地改变反应条件,相同的起始原料既可以用于改进二氢三嗪骨架的合成,也可以用于一种新颖的、同类首创的多组分反应(MCR),从而一步合成具有挑战性的5-氨基咪唑核。还报道了另一种利用胍的同类首创的多组分反应,以制备2,5-氨基咪唑。