申请人:Kunishima Munetaka
公开号:US09126954B2
公开(公告)日:2015-09-08
To provide: a hydroxy group protecting agent which is stable and easy to use, does not have carcinogenicity, a tearing property or the like, and is inexpensive; and a hydroxy group protection method which enables the protection of a hydroxy group under acidic conditions.
[Solution] A hydroxy group protecting agent in which at least one protecting group is bound to a nitrogen-containing electron-withdrawing heterocyclic ring through any one of an oxygen atom, a sulfur atom and a nitrogen atom. The heterocyclic ring is a triazine ring or the like, and the protecting group is a benzyl group or the like. Specifically, the hydroxy group protecting agent is 2,4,6-tribenzyloxy-1,3,5-triazine, 2,4,6-tris(4-methoxybenzyloxy)-1,3,5-triazine or the like. In addition, 2,4,6-tris(t-butoxy)-1,3,5-triazine or the like can also be used. For protecting a hydroxy group, a compound of interest which has a hydroxy group is reacted with the hydroxy group protecting agent under acidic conditions.
提供:一种稳定易用、不具有致癌性、撕裂性或类似特性且价格低廉的羟基保护剂;以及一种羟基保护方法,可在酸性条件下保护羟基。
【解决方案】一种羟基保护剂,其中至少一个保护基通过氧原子、硫原子和氮原子中的任意一个与含氮的电子吸引杂环环上结合。所述杂环是三嗪环或类似环,所述保护基是苄基或类似基团。具体而言,所述羟基保护剂是2,4,6-三苄氧基-1,3,5-三嗪、2,4,6-三(4-甲氧基苄氧基)-1,3,5-三嗪或类似物。此外,也可以使用2,4,6-三(叔丁氧基)-1,3,5-三嗪或类似物。为了保护羟基,将具有羟基的化合物在酸性条件下与羟基保护剂反应。