作者:Xianhua Pan、Xiaohu Tao、Libo Ruan、Yiming Li、Wenhua Ou、Feng Liu
DOI:10.3184/174751911x13237056070415
日期:2011.12
An efficient synthesis of (R)-3-aminothiolane is described based on a one-pot tandem hydroxyl activation-intramolecular cyclisation of Ts-protected-D-methioninol in the presence of methanesulfonyl chloride/pyridine. Removal of the tosyl group then gave (R)-3-aminothiolane in good yield. (R)-3-Aminothiolane derivatives are important building blocks for the synthesis of biologically active compounds
在甲磺酰氯/吡啶存在下,基于 Ts 保护的 D-蛋氨醇的一锅串联羟基活化-分子内环化,描述了 (R)-3-氨基硫烷的有效合成。除去甲苯磺酰基,然后以良好的收率得到(R)-3-氨基硫杂环戊烷。(R)-3-Aminothiolane 衍生物是合成生物活性化合物的重要组成部分。