中国药学（英文版）
中國藥學（英文版）
중국약학（영문판）
JOURNAL OF CHINESE PHARMACEUTICAL SCIENCES
2007年
1期
43-46
,共4页
氧桥%双环氮杂糖%双环硫杂糖%关环反应
氧橋%雙環氮雜糖%雙環硫雜糖%關環反應
양교%쌍배담잡당%쌍배류잡당%관배반응
Oxy-bridge%Bicyclic azasugar%Bicyclic thiosugar%Ring-closure
目的 发展一种简洁合成具有新型骨架的双环氮杂糖和硫杂糖的新方法.方法 化合物1的两个伯羟基先在吡啶中用对甲苯磺酰氯保护,接下来用硫化钠和伯胺关环高收率地生成氧桥双环分子.结果 经几步反应成功地从L-山梨糖合成了三种双环氮杂糖和硫杂糖.结论 本方法提供了一种合成具有潜在糖苷酶抑制活性的氧桥双环氮杂糖和硫杂糖的有效途径.
目的 髮展一種簡潔閤成具有新型骨架的雙環氮雜糖和硫雜糖的新方法.方法 化閤物1的兩箇伯羥基先在吡啶中用對甲苯磺酰氯保護,接下來用硫化鈉和伯胺關環高收率地生成氧橋雙環分子.結果 經幾步反應成功地從L-山梨糖閤成瞭三種雙環氮雜糖和硫雜糖.結論 本方法提供瞭一種閤成具有潛在糖苷酶抑製活性的氧橋雙環氮雜糖和硫雜糖的有效途徑.
목적 발전일충간길합성구유신형골가적쌍배담잡당화류잡당적신방법.방법 화합물1적량개백간기선재필정중용대갑분광선록보호,접하래용류화납화백알관배고수솔지생성양교쌍배분자.결과 경궤보반응성공지종L-산리당합성료삼충쌍배담잡당화류잡당.결론 본방법제공료일충합성구유잠재당감매억제활성적양교쌍배담잡당화류잡당적유효도경.
Aim To develop a concise method for the synthesis of bicyclic azasugar and thiosugar with novel scaffold. Methods The two primary hydroxyl groups of compound 1 were selectively protected with tosyl cloloride in pyridine, followed by ring-closure with sodium sulfide or primary amine to form the oxy-bridged bicyclic molecules in good yields. Results Two bicyclic azasugars and a thiosugar were produced from L-sorbose in several steps. Conclusion The described procedures provide an efficient method to synthesize bicyclic azasugar and thiosugar with novel scaffold as potential glycosidase inhibitors.
