吲哚里西定167B前体的合成

Formal Synthesis of Indolizidine 167B Precursor

以Boc-L-脯氨酸为原料,进行Weinreb酰胺化反应、乙炔格氏试剂的取代反应、分子内氮参与的1,4加成反应以及分子间迈克尔加成反应。用4步反应得到的46.74%的产率合成了含有2个手性中心的重要中间体。

The formal synthesis of Indolizidine 167B was achieved from Boc-L-proline through the substitu- tion reaction of Ethynyl magnesium bromide,intramolecular aza-Micheal addition reaction and intermolecu- lar Micheal addition reaction. The key midbody of Indolizidine 167B with two chiral centers was obtained at a rate of 46.74% through the 4 reactions.