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Palladium-catalyzed C-3 desulfitative arylation of indolizines with sodium arylsulfinates and arylsulfonyl hydrazides

机译:钯 - 催化吲哚酸钠和芳基磺酰肼的吲哚嗪的C-3脱硫淀粉

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Derivatized indolizines were efficiently prepared by direct C-3 arylation of indolizines using sodium arylsulfinates and arylsulfonyl hydrazides. Pd-catalyzed desulfitative C-3 arylation with sodium arylsulfinates was achieved with the assistance of peroxides, and the catalytic efficiency was promoted by N-containing ligands. Arylsulfonyl hydrazides were also successfully applied in Pd-catalyzed desulfitative C-3 arylation with indolizines, and the side homocoupling reactions can be restrained in the component solvent under milder conditions. Various derivatives were synthesized in good yields by both methods, offering expedient protocols for the synthesis of C-3 functionalized indolizine molecules.
机译:通过使用淀粉磺酸钠和芳基磺酰基肼直接C-3芳酸酯的C-3芳基化,有效地制备衍生的吲哚吲硫。在过氧化物的辅助下,实现了PD催化的脱硫C-3芳磺酸钠芳基磺酸盐,并通过含N含N的配体促进催化效率。用吲硫胺成功地应用于PD催化的脱硫C-3芳基化合物中的芳基磺酰基肼,并且可以在较温和的条件下抑制侧同性耦合反应。两种方法以良好的产量合成各种衍生物,为合成C-3官能化吲硫胺分子提供有利方案。

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