METHOD FOR PRODUCING DIPEPTIDE DERIVATIVE CONTAINING DISUBSTITUTED AMINO ACID RESIDUE

摘要

A method for producing a dipeptide that has a protected N-terminal and is represented by formula (1) or a salt of the dipeptide, said method comprising condensing an α-monosubstituted amino acid that has a protected N-terminal and is represented by formula (2) or glycine or a salt thereof with a disubstituted amino acid that is represented by formula (3) or a salt thereof in the presence of a condensing agent [in each of the formulae, substituents are as defined in the description or the like].;

主权项

1. A method for producing an N-terminal protected dipeptide represented by the following formula (1) or a salt thereof:wherein X represents a protecting group for an amino group,R1 represents a side chain of an α-monosubstituted amino acid, or a hydrogen atom,wherein the side chain is optionally protected,R2 represents a group bonded to R1 to form the side chain, or a hydrogen atom, andRa2 and Rb2 each independently represent an alkyl group optionally having a substituent, an alkenyl group optionally having a substituent, an alkynyl group optionally having a substituent, or an aralkyl group optionally having a substituent,
the production method comprising condensing an N-terminal protected α-monosubstituted amino acid or glycine represented by the following formula (2), or a salt of the amino acid or glycine:wherein X, R1, and R2 are as defined for X, R1, and R2, respectively, in the formula (1),
with a disubstituted amino acid represented by the following formula (3) or a salt thereof:wherein Ra2 and Rb2 are as defined for Ra2 and Rb2, respectively, in the formula (1) in the presence of a condensing agent.