Amine hydrochloride having maleimide group, and method for producing same
AssigneeNof Corporation
InventorsAiko KAWADA, Shuhei KINOSHITA, Takato KIMURA, Yuuki ISOBE
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Abstract
An amine protector having a maleimide group represented by the formula (2) as defined herein is deprotected with trifluoroacetic acid to obtain an amine trifluoroacetate having a maleimide group represented by the formula (3) as defined herein, and the amine trifluoroacetate is mixed with an organic solvent solution of hydrogen chloride to perform salt exchange to obtain an amine hydrochloride having a maleimide group represented by the formula (1) as defined herein.
Claims9
A method for producing an amine hydrochloride having a maleimide group represented by a formula (1), the method comprising:
- a step (a) of deprotecting an amine protector having a maleimide group represented by the following formula (2) with trifluoroacetic acid to obtain an amine-trifluoroacetate having a maleimide group represented by the following formula (3);
- and
- a step (b) of mixing the amine-trifluoroacetate obtained in the step (a) with an organic solvent solution of hydrogen chloride to perform salt exchange to obtain the amine hydrochloride having the maleimide group represented by the formula (1):
- wherein, in the formula (1), L represents a linker connecting the maleimide group and an amino group,
- wherein, in the formula (2), L represents a linker connecting the maleimide group and a protected amino group, and R represents a protecting group for the amino group,
- wherein, in the formula (3), L represents a linker connecting the maleimide group and an amino group.
An amine hydrochloride having a maleimide group represented by the following formula (1), comprising:
- a hydrogen chloride adduct of an amine hydrochloride represented by the following formula (11), wherein
- a content of the hydrogen chloride adduct is 0.001% by mass or more and 2.5% by mass or less:
- wherein in the formula (1) and the formula (11), L represents a linker connecting the maleimide group and an amino group.
Dependencies are inferred from the claim text.