公开(公告)号：EP2370450A1

公开(公告)日：2011-10-05

申请号：EP09763860.5

申请日：2009-11-25

申请人： Roche Diagnostics GmbH ,  F. Hoffmann-La Roche AG

发明人： HEINDL, Dieter ,  KESSLER, Dirk ,  ROESLER, Angelika ,  SEIDEL, Christoph ,  THUER, Wilma

IPC分类号： C07F9/24 ,  C08G79/04

CPC分类号： G01N33/5308 ,  C07F9/6552 ,  C07F9/65586 ,  Y02P20/55

摘要： The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula (1) are produced in a stereocontrolled manner.

摘要翻译： 化合物的三价磷原子与试剂反应，形成稳定的磷酸酯模拟物或说明符。 具有含至少一个提供有保护基团的羟基残基的磷原子的亚磷酰胺为此目的与游离羟基反应：在第一个合成循环中，羟基通过可裂解或不可裂解与固体载体连接 连接。 在进一步的合成循环中，羟基通过从生长中的寡聚体上切下保护基而产生。 这导致形成与叠氮化物反应的亚磷酸三酯。 通过选择合适的具有确定的立体构象的合成单体，以立体控制的方式制备式（1）的化合物。