公开(公告)号：US08853132B2

公开(公告)日：2014-10-07

申请号：US14026936

申请日：2013-09-13

Applicant: Roche Diagnostics Operations, Inc.

Inventor： Dieter Heindl ,  Dirk Kessler ,  Angelika Roesler ,  Christoph Seidel ,  Wilma Thuer

IPC: C07F9/6558 ,  G01N33/53 ,  C07F9/655

CPC classification number: G01N33/5308 ,  C07F9/6552 ,  C07F9/65586 ,  Y02P20/55

Abstract: 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.

Abstract translation: 使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物。 具有至少一个含有保护基团的羟基残基的磷原子的亚磷酰胺与该游离羟基反应：在第一个合成循环中，羟基通过可裂解或不可切割的方式与固体支持物连接 接头。 在进一步的合成循环中，通过从生长的低聚物中切割保护基而产生羟基。 这导致形成与叠氮化物反应的亚磷酸三酯。 通过选择具有定义的立体定构的合成合成单体，以立体控制的方式制备式1的化合物。

公开(公告)号：US20140045719A1

公开(公告)日：2014-02-13

申请号：US14026936

申请日：2013-09-13

Applicant: ROCHE DIAGNOSTICS OPERATIONS, INC.

Inventor： Dieter Heindl ,  Dirk Kessler ,  Angelika Roesler ,  Christoph Seidel ,  Wilma Thuer

IPC: G01N33/53 ,  C07F9/655

CPC classification number: G01N33/5308 ,  C07F9/6552 ,  C07F9/65586 ,  Y02P20/55

Abstract: 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.

Abstract translation: 使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物。 具有至少一个含有保护基团的羟基残基的磷原子的亚磷酰胺与该游离羟基反应：在第一个合成循环中，羟基通过可裂解或不可切割的方式与固体支持物连接 接头。 在进一步的合成循环中，通过从生长的低聚物中切割保护基而产生羟基。 这导致形成与叠氮化物反应的亚磷酸三酯。 通过选择具有定义的立体定构的合成合成单体，以立体控制的方式制备式1的化合物。