Abstract

Two different amino piperazine derivatives bearing various halogen groups were synthesized in high yields and explored in further transformations. Reacting these amino piperazines with various sulfonyl chlorides yielded eight different sulfonamides. Additionally, eight different urea derivatives have been prepared by treating these amino piperazines with isocyanates. Finally, we were able to take advantage of the aryl bromide functionality present in the parent amino piperazines by subjecting them to the Suzuki coupling with phenylboronic acid. Overall, we developed a strategy to diversify the amino piperazine core and obtained a small library of potentially bioactive piperazine derivatives.

摘要

以高产率合成了两种带有不同卤素基团的不同氨基哌嗪衍生物，并在进一步的转化中进行了探索。将这些氨基哌嗪与各种磺酰氯反应产生八种不同的磺酰胺。此外，通过用异氰酸酯处理这些氨基哌嗪，制备了八种不同的脲衍生物。最后，我们能够利用母体氨基哌嗪中存在的芳基溴官能团，将它们与苯硼酸进行 Suzuki 偶联。总体而言，我们开发了一种使氨基哌嗪核心多样化的策略，并获得了一个小的潜在生物活性哌嗪衍生物库。