Chiral 4-boronophenylalanine (BPA) derivative and method for producing same, and method for producing ¹⁸F-labeled BPA using said derivative

摘要

Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing ¹⁸F-2-fluoro-4-borono-L-phenylalanine (¹⁸F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR³R⁴, BX₃⁻ or BX₃⁻M⁺ (wherein X represents a halogen atom, and M⁺ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R₁ represents a hydrogen atom or a protecting group PG1; R₂ represents a hydrogen atom or a protecting group PG2; R₃ and R₄ independently represent OH, or R³, R⁴ and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO₂, NH₂, Sn(R⁶)₃, N═N—NR⁷R⁸, OSO₂R⁹, NR¹⁰R¹¹, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare ¹⁸F-labeled BPA.