Method for removing FMOC group

摘要

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 C1-8 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.

主权项

1. A method of removing an Fmoc group, comprising:
mixing an amino group-containing compound protected by an Fmoc group, a base, and a compound represented by formula (I):
HS-L-COOH  (I) where L is a C1-8 alkylene group optionally having at least one substituent, to obtain a reaction mixture comprising an amino group-containing compound and a compound represented by formula (II):
Fm—S-L-COOH  (II) where Fm is a 9-fluorenylmethyl group; and washing the reaction mixture with a basic aqueous solution such that the compound represented by the formula (II) is removed; wherein the amino group-containing compound protected by an Fmoc group, and the amino group-containing compound, do not have a free carboxy group.