1,5-苯并硫氮杂-α-氨基-β-内酰胺衍生物的合成及立体结构(Ⅱ)

Synthesis and Steric Structure of α-Amino-β-lactam Derivatives of 1,5-Benzothiazepines

用一种甘氨酸 N-端保护试剂和 1 ,5 -苯并硫氮杂反应 ,合成了 5个 1 ,5 -苯并硫氮杂 -α-氨基 -β-内酰胺衍生物 ,其结构经元素分析、 1 H NMR,MS和 IR确证 .用 X射线衍射法确定了产物的立体结构 ,结果表明 ,该反应具有立体专一性 ,四元环上的两个取代基位于环的同侧 ,为顺式结构 ,产物分子中的七元环为稳定的类椅式构象 .

Benzothiazepines reacted with a new N-protected agent of glycine to give the title compounds. The configuration and conformation of the products were determined by X-ray crystal analysis. The results also revealed that the reaction was stereospecific. The two substituents at β-lactam were on the same side, the seven-membered ring was in chair-like conformation.