申请人:Biomira, Inc.
公开号:US05527891A1
公开(公告)日:1996-06-18
A stereodirected process for synthesizing .alpha.-N-acetylgalactosaminides from N-acetylgalactosamine which, in a preferred embodiment, comprises: reacting N-acetylgalactosamine with a dialkyl acetal of an aldehyde or ketone to form a 4,6-O-alkylidene derivative; reacting said 4,6-O-alkylidene derivative with a protecting group compound to attach a protecting group selectively to 3-OH of said derivative to form a 3-O-protected derivative; reacting said 3-O-protected derivative with an anomeric group to form a glycosyl donor; reacting said glycosyl donor with an alcohol to form an N-acetylgalactosaminide.
一种立体定向的合成α-N-乙酰半乳糖氨苷的方法,从N-乙酰半乳糖胺开始,在优选实施例中,包括以下步骤:将N-乙酰半乳糖胺与醛或酮的二烷基缩醛反应,形成4,6-O-烷基亚甲基衍生物;将所述4,6-O-烷基亚甲基衍生物与保护基化合物反应,选择性地将保护基连接到所述衍生物的3-OH上,形成3-O-保护衍生物;将所述3-O-保护衍生物与环异构基反应,形成糖基供体;将所述糖基供体与醇反应,形成N-乙酰半乳糖氨苷。