Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: application to four-step synthesis of gabazine (SR-95531)
作者:Navnath Gavande、Graham A. R. Johnston、Jane R. Hanrahan、Mary Chebib
DOI:10.1039/c0ob00004c
日期:——
Microwave-enhanced, highly efficient protocols for the synthesis of synthetically and biologically important 2,3,6-trisubstituted pyridazine architectures have been developed by sequential amination/Suzuki coupling/alkylation reactions. This powerful strategy is an economical and highly chemoselective protocol for the synthesis of diversified pyridazines. The total synthesis of gabazine (SR-95531)
微波增强的,高效的合成和生物学上重要的2,3,6-三取代合成方案 哒嗪通过顺序胺化/ Suzuki偶联/烷基化反应已经开发出各种结构。这种强大的策略是用于合成多种哒嗪的经济且高度化学选择性的方案。川ab嗪的全合成(SR-95531)可通过四个步骤采用多功能策略实现,总收率达到73%。