An efficient direct C(sp³)−H (hetero)arylation of of 5H-imidazo[2,1-a]isoindole scaffolds with arylbromides is described under Pd catalysis affording a wide range of the corresponding arylated compounds on the benzylic position in good yields. This methodology was applied to prepare a neurotransmitter Neuropeptide S antagonist analog illustrating that this methodology can be used for the late stage functionalization to obtain molecules of interest.

中文翻译：

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钯催化 5H-咪唑并[2,1-a]异吲哚支架与芳基溴的直接 C(sp3)−H 芳基化


描述了在 Pd 催化下，5H-咪唑并[2,1-a]异吲哚支架与芳基溴的有效直接 C(sp ³ )−H（杂）芳基化，提供了各种相应的芳基化化合物位于苯甲基位置上，产率良好。该方法用于制备神经递质神经肽S拮抗剂类似物，说明该方法可用于后期功能化以获得感兴趣的分子。