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1. 发明申请

WO0149674A3 GLYCOSIDASE INHIBITORS AND PREPARATION THEREOF 审中-公开
标题翻译：甘氨酸酶抑制剂及其制备方法
公开(公告)号：WO0149674A3
公开(公告)日：2001-11-29
申请号：PCT/CA0100010
申请日：2001-01-05
申请人： UNIV FRASER SIMON , PINTO BRIAN M , JOHNSTON BLAIR D , GHAVAMI AHMAD
发明人： PINTO BRIAN M , JOHNSTON BLAIR D , GHAVAMI AHMAD
IPC分类号： C07D333/32 , A61K31/33 , A61K31/381 , A61K31/40 , A61P3/08 , A61P3/10 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07B61/00 , C07D207/12 , C07D333/46 , C07D345/00 , C07D405/06 , C07D409/06 , C07D421/06 , C07D497/04 , C07D211/04 , C07D211/92 , C07D335/00
CPC分类号： C07D333/46 , C07D207/12 , C07D345/00
摘要： A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having formula (I). The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions. In an alternative embodiment of the invention, the cyclic sulfate may be similarly reacted with a 6-membered ring sugar containing a heteroatom (X) to yield a compound having formula (XII).
摘要翻译：一种用于合成具有式（I）的Salacinol，其立体异构体和非天然存在的硒和氮类似物的方法。这些化合物可能用作糖苷酶抑制剂。合成方案包括使环硫酸盐与含有杂原子（X）的5元环糖反应。杂原子优选包含硫，硒或氮。环状硫酸盐和环糖试剂可以容易地从碳水化合物前体如D-葡萄糖，L-葡萄糖，D-木糖和L-木糖制备。通过在5元环糖上的杂原子的亲核攻击来打开环状硫酸盐来制备目标化合物。所得的杂环化合物具有包含杂原子阳离子和硫酸根阴离子的稳定的内盐结构。合成方案以有限的副反应以中等到良好的产率产生目标化合物的各种立体异构体。在本发明的一个替代实施方案中，环状硫酸盐可以类似地与含有杂原子（X）的6元环糖反应，得到具有式（XII）的化合物。

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