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 18 F-2-fluoro-4-borono-L-phenylalanine ( 18 F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR 3 R 4 , BX 3 - or BX 3 - M + (wherein X represents a halogen atom, and M + represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R 1 represents a hydrogen atom or a protecting group PG1; R 2 represents a hydrogen atom or a protecting group PG2; R 3 and R 4 independently represent OH, or R 3 , R 4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO 2 , NH 2 , Sn(R 6 ) 3 , N=N-NR 7 R 8 , OSO 2 R 9 , NR 10 R 11 , a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18 F-labeled BPA.