申请人:Ajinomoto Co., Inc.
公开号:EP2518041A1
公开(公告)日:2012-10-31
Provided is a protecting reagent which can undergo deprotection in high yield even under acidic conditions in organic synthesis, e.g., peptide synthesis, and which enables high-purity products to be obtained. The protecting reagent is a benzyl compound represented by formula(I), which has only one hydroxyl group substituted by an organic group comprising an aliphatic hydrocarbon group and having 14 or more carbon atoms in total. [In formula(I), Y represents a hydroxyl group or -NHR (R represents a hydrogen atom, an alkyl, or an aralkyl); Ra represents an organic comprising an aliphatic hydrocarbon group, the total number of carbon atoms of the organic group being 14 or more; the n Rbs each independently represents a C1-6 alkoxy, a halogen atom, or C1-6 alkyl optionally substituted by one or more halogen atoms; and n is an integer of 0-4.]
本发明提供了一种保护试剂,它在有机合成(如肽合成)中即使在酸性条件下也能高产率地进行脱保护,并能获得高纯度产品。保护试剂是由式(I)表示的苄基化合物,它只有一个羟基,被由脂肪族烃基组成的有机基团取代,总共有 14 个或更多的碳原子。[在式(I)中,Y 代表羟基或-NHR(R 代表氢原子、烷基或芳烷基);Ra 代表包含脂族烃基的有机物,该有机物的碳原子总数为 14 个或更多;n 个 Rbs 各自独立地代表 C1-6 烷氧基、卤素原子或任选被一个或多个卤素原子取代的 C1-6 烷基;n 为 0-4 的整数。]