A tyrosine derivative represented by the following formula: wherein both R 1 are hydrogen atoms, or one R 1 is a hydrogen atom and one R 1 is a protective group for the amino group selected from a carbamate-type protective group, a sulfonamide-type protective group, an amide-type protective group, a benzyl-type protective group or a triphenylmethyl group, or both R 1 are the protective groups for the amino group or form a cyclic protective group including in its ring the nitrogen atom; R 2 is a hydrogen atom or an ester protective group for the carboxy group; R 3 is a hydrogen atom or a C 1-6 alkyl group; R 4 is a halogen atom, a hydroxy group, a C 1-6 alkyl group, a C 1-6 halogenated alkyl group, an amino group, a mono(C 1-6 alkyl)amino group, a di(C 1-6 alkyl) amino group, a C 6-12 aryl group optionally having substituent α, a heterocyclic group optionally having substituent α, a C 1-6 alkoxy group, a C 1-6 alkylthio group, a C 1-6 halogenated alkoxy group or a C 7-13 aralkyloxy group optionally having substituent α; A is -(CH 2) l -[Z(CH 2) m] n - wherein Z is an amino group, an ether group, a thioether group, a carbonyl group, a thionyl group, an ester group, an amide group, a urea group or a thiourea group; 1 is an integer of not less than 1 and not more than 6; m is an integer of not less than 1 and not more than 4; and n is an integer of not less than 0 and not more than 4; X is a leaving group selected from the group consisting of a chlorine atom, a bromine atom, an iodine atom, a methanesulfonyloxy group, a trifluoromethanesulfonyloxy group, a chloromethanesulfonyloxy group, an ethanesulfonyloxy group, a benzenesulfonyloxy group and a toluenesulfonyloxy group; substituent α is one or more substituents selected from the group consisting of a halogen atom, a hydroxy group, a cyano group, a thiol group, an amino group, a mono(C 1-6 alkyl) amino group, a di(C 1-6 alkyl) amino group, a C 1-6 alkyl group, a C 1-6 alkoxy group, a C 1-6 halogenated alkyl group and a C 1-6 alkylthio group; provided that the position of R 4 is para to the position of the X-A-O- group. both R 1 are hydrogen atoms, or one R 1 is a hydrogen atom and one R 1 is a protective group for the amino group selected from a carbamate-type protective group, a sulfonamide-type protective group, an amide-type protective group, a benzyl-type protective group or a triphenylmethyl group, or both R 1 are the protective groups for the amino group or form a cyclic protective group including in its ring the nitrogen atom; R 2 is a hydrogen atom or an ester protective group for the carboxy group; R 3 is a hydrogen atom or a C 1-6 alkyl group; R 4 is a halogen atom, a hydroxy group, a C 1-6 alkyl group, a C 1-6 halogenated alkyl group, an amino group, a mono(C 1-6 alkyl)amino group, a di(C 1-6 alkyl) amino group, a C 6-12 aryl group optionally having substituent α, a heterocyclic group optionally having substituent α, a C 1-6 alkoxy group, a C 1-6 alkylthio group, a C 1-6 halogenated alkoxy group or a C 7-13 aralkyloxy group optionally having substituent α; A is -(CH 2) l -[Z(CH 2) m] n - wherein Z is an amino group, an ether group, a thioether group, a carbonyl group, a thionyl group, an ester group, an amide group, a urea group or a thiourea group; 1 is an integer of not less than 1 and not more than 6; m is an integer of not less than 1 and not more than 4; and n is an integer of not less than 0 and not more than 4; X is a leaving group selected from the group consisting of a chlorine atom, a bromine atom, an iodine atom, a methanesulfonyloxy group, a trifluoromethanesulfonyloxy group, a chloromethanesulfonyloxy group, an ethanesulfonyloxy group, a benzenesulfonyloxy group and a toluenesulfonyloxy group; substituent α is one or more substituents selected from the group consisting of a halogen atom, a hydroxy group, a cyano group, a thiol group, an amino group, a mono(C 1-6 alkyl) amino group, a di(C 1-6 alkyl) amino group, a C 1-6 alkyl group, a C 1-6 alkoxy group, a C 1-6 halogenated alkyl group and a C 1-6 alkylthio group; provided that the position of R 4 is para to the position of the X-A-O- group.