申请人:Ajinomoto Co., Inc.
公开号:US20140296483A1
公开(公告)日:2014-10-02
The present invention relates to a method of removing an Fmoc group, including a step of mixing a compound represented by the formula (I):
HS-L-COOH (I)
wherein L is a C
1-8
alkylene group optionally having substituent(s), an amino group-containing compound protected by an Fmoc group, and a base to give a reaction mixture containing a compound represented by the formula (II):
Fm-S-L-COOH (II)
wherein Fm is a 9-fluorenylmethyl group, and L is as mentioned above, and an amino group-containing compound, and a step of removing the compound represented by the formula (II) by washing the obtained reaction mixture with a basic aqueous solution. According to the present invention, a removal method of Fmoc group, which can remove a dibenzofulvene derivative as a byproduct with ease, can be provided.
本发明涉及一种去除Fmoc基团的方法,包括混合式化合物(I)的步骤:HS-L-COOH(I),其中L是一个C1-8烷基链,可选地具有取代基,一种被Fmoc基团保护的氨基化合物和一种碱,以得到一种反应混合物,其中包含一种化合物,其由式(II)表示:Fm-S-L-COOH(II),其中Fm是9-芴甲基基团,L如上所述,还包括一种氨基化合物,以及通过用碱性水溶液洗涤所得到的反应混合物,去除由式(II)表示的化合物。根据本发明,可以提供一种可以轻松去除二苯并富烯衍生物作为副产物的Fmoc基团去除方法。