Joyann S. Donaldson*, Matthew Del Bel, John Braganza, Sujin Cho-Schultz, Mingying He, Bryan Li, Congjun Liu, Jean Matthews, Sajiv K. Nair, Martha Ornelas, Feng Shi, Chengfu Xie, Qing Zhang and Ru Zhou,
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Synthesis of Fused Bicyclic [1,2,4]-Triazoles from Amino Acids
A 3-step modular procedure combining carboxylic acids with acyl hydrazines provides access to medicinally relevant [1,2,4]-fused triazoles. Good to excellent yields are achieved with tolerance of aliphatic and aryl substituents as well as 5-, 6-, and 7-membered rings for the fused ring. Conditions that can avoid column chromatography and be applicable for both small scale discovery efforts as well as large scale development processes are demonstrated within.
期刊介绍:
Journal of Organic Chemistry welcomes original contributions of fundamental research in all branches of the theory and practice of organic chemistry. In selecting manuscripts for publication, the editors place emphasis on the quality and novelty of the work, as well as the breadth of interest to the organic chemistry community.