1,5-苯并硫氮杂-α氨基-β-内酰胺的合成

Synthesis of α-Amino-β-lactam Derivatives of 1,5-Benzothiazepine

甘氨酸和邻苯二甲酸酐反应 ,首先得到邻苯二甲酰基保护的甘氨酰氯 ,继而和 1 ,5 -苯并硫氮杂在三乙胺的存在下作用 ,得到 6个 1 ,5 -苯并硫氮杂 -α氨基 -β-内酰胺衍生物。所有产物的结构均经 1H NMR、IR、MS。

N-protected glycine was prepared by the reaction of glycine and phthalic anhydride without any solvent. Then, it reacted with 1,5-benzothiazepines 4a-f in the presence of triethylamine to form a series of corresponding α-amino-β-lactam derivatives. The structures of the products were confirmed by 1H NMR, MS, IR and elemental analysis.