Synthesis of Substituted 6,7-Dihydro-5H-pyrrolo2,3-cpyridazines/pyrazines via Catalyst-Free Tandem Hydroamination-Aromatic Substitution

摘要

Herein, we report an efficient and operationally simple synthesis of 6,7-dihydro-5H-pyrrolo2,3-cpyridazines and 6,7-dihydro-5H-pyrrolo2,3-bpyrazines via a tandem hydroamination-SNAr sequence that makes use of mild reagents under catalyst-free conditions in moderate to high yields. This chemistry expands the known scope of pyridazine/pyrazine chemistry and can be applied toward the synthesis of novel drug-like molecules with favorable bioactivity and pharmacokinetic properties.