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.
化合物中的三价
磷原子与试剂反应,形成稳定的
磷酸盐类似物或特异性物质。为此,具有至少一个含有保护基的氢氧基的含
磷原子的
磷酰胺酯与自由氢氧基反应:在第一个合成循环中,通过可裂解或不可裂解的连接剂将氢氧基与固体支持物连接。在进一步的合成循环中,通过从生长寡聚物中裂解保护基来创建氢氧基。这导致形成
磷酸三酯,然后与
叠氮化物反应。通过选择合适的单体进行合成,这些单体具有定义的立体构型,从而以立体控制的方式产生式(1)的化合物。