A convenient synthesis of 8-substituted indolizines as precursors to 5-substituted cycl{3.2.2}azine derivatives
作者:Jonathan O. Smith、Braja K. Mandal
DOI:10.1002/jhet.5570340511
日期:1997.9
provides 8-substituted indolizines in good yields. Treatment of 8-substituted indolizines with dimethyl acetylenedicarboxylate, in the presence of palladium-on-carbon, provides novel 5-substituted cycl3.2.2) derivatives.
通过两步法描述了8取代的吲哚嗪的合成方法,其中将含叔丁基的1,4-二酮与三烷基甲硅烷基保护的吡咯进行环缩合反应,从而以比苯甲酸更高的收率提供5,8-二取代的吲哚嗪。与未保护的吡咯反应相同。通过用85%的磷酸处理从吲哚嗪5-位上裂解叔丁基,以良好的产率提供了8-取代的吲哚嗪。在碳载钯存在下,用乙炔二羧酸二甲酯处理8-取代的吲哚嗪,可提供新颖的5-取代的环(3.2.2)衍生物。