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公开(公告)号：US5700916A
公开(公告)日：1997-12-23
申请号：US281167
申请日：1994-07-27
IPC分类号： C07H1/00 , B01J31/02 , C07H3/00 , C07H3/02 , C07H3/04 , C07H3/06 , C07H11/00 , C07H15/14 , C07H15/18 , C07H15/203 , C07H17/04 , C07H19/04 , C08B37/00 , C40B50/08 , C07G3/00 , C07H15/00
CPC分类号： C07H15/14 , C07H11/00 , C07H15/18 , C07H15/203 , C07H17/04 , C07H19/04 , C07H3/04 , C07H3/06 , B01J2219/00599 , C07B2200/11 , C40B50/08
摘要： The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage of the discovery that the relative reactivity of glycoside residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. In another aspect of the invention, the reactivity of activated anomeric sugar sulfoxides is utilized in a solid phase method for the formation of glycosidic linkages. The methods disclosed may be applied to the preparation of specific oligosaccharides and other glycoconjugates, as well as to the preparation of glycosidic libraries comprising mixtures of various oligosaccharides, including glycoconjugates, which can be screened for biological activity.
摘要翻译： 本发明涉及允许快速构建寡糖和其它糖缀合物的方法。 公开了在单一步骤中在溶液中形成多个糖苷键的方法。 本发明利用了可以控制含有异聚亚砜和亲核官能团的糖苷残基的相对反应性的发现。 在本发明的另一方面，活化的端基异构糖亚砜的反应性用于形成糖苷键的固相方法。 所公开的方法可以应用于制备特异性寡糖和其它糖缀合物，以及制备包含可以筛选生物活性的各种寡糖（包括糖缀合物）的混合物的糖苷文库。
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公开(公告)号：US5508463A
公开(公告)日：1996-04-16
申请号：US214368
申请日：1994-03-17
CPC分类号： C07F9/65515 , C07F9/4006 , C07F9/4018 , C07F9/4056
摘要： Novel .alpha.-aminophosphonates are provided along with processes and intermediates for their preparation. In preferred embodiments, scalemic .alpha.-aminophosphonates are prepared by the stereoselective addition of phosphite salts to chiral imines.
摘要翻译： 提供新的α-氨基膦酸盐以及其制备方法和中间体。 在优选的实施方案中，通过立体选择性将亚磷酸盐加成到手性亚胺中来制备鳞片状α-氨基膦酸酯。
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公开(公告)号：US5824809A
公开(公告)日：1998-10-20
申请号：US633952
申请日：1996-04-15
CPC分类号： C07F9/65515 , C07F9/4006 , C07F9/4018 , C07F9/4056
摘要： Novel .alpha.-aminophosphonates are provided along with processes and intermediates for their preparation. In preferred embodiments, scalemic .alpha.-aminophosphonates are prepared by the stereoselective addition of phosphite salts to chiral imines.
摘要翻译： 提供新的α-氨基膦酸盐以及其制备方法和中间体。 在优选的实施方案中，通过立体选择性将亚磷酸盐加成到手性亚胺中来制备鳞片状α-氨基膦酸酯。
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