摘要/Abstract

有氧条件下以NH₄OAc/ N, N-二甲基甲酰胺(DMF)组合为氰源, 发展了Ag/Cu介导芳基羧酸脱羧的氰化反应, 并进一步实现了以该方法为关键步骤的吡仑帕奈(perampanel)合成. 初步的机理研究表明, 产物中的“CN”来源于NH₄ ⁺/ DMF组合, 催化体系中的Cu决定着反应的发生, Ag有利于反应的转化.
关键词: 脱羧, 芳基腈化物, 有氧条件
A Ag/Cu-mediated decarboxylative cyanation of aryl carboxylic acids has been well established using NH₄OAc/ N, N-dimethylformamide (DMF) as a combined cyanide source under aerobic conditions, and the synthesis of perampanel was further realized with this method as the key step. Preliminary mechanistic investigation indicated the “CN” of desired products was from the combination of DMF and ammonium salt. Cu in the catalytic system was essential for the process, whereas Ag was beneficial for the transformation.
Key words: decarboxylation, aryl nitrile, aerobic conditions


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