Disclosed is a derivative of chiral 4-Boronophenylalanine (BPA), a manufacturing method thereof and a manufacturing method of 18F-2-Fluoro-4-Borono-L-phenylalanine using said derivative. A compound prepared via the instant disclosure is represented by the following equation.Wherein, R represents BR3R4, BX3-, or BX3-M+ (wherein the X is a halogen, M+ is a monovalent ion which may be a monoatomic cation, a polyatomic cation, or a complex cation)； R1 represents hydrogen or protecting group PG1； R2 represents hydrogen or protecting group PG2； R3 and R4 represent OH, respectively, or both form a ring together with B to serve as a protecting group； Y represents halogen, NO2, NH2, Sn(R6)3, N=N-NR7R8, OSO2R9, NR10R11, substituted or not substituted iodo-phenyl, substituted or not substituted iodo-heterocyclyl (wherein, R6 represents alkyl (1≦C≦7)； R7 and R8, being the same or different, represent hydrogen, alkyl (1≦C≦7), alkyl (1≦C≦7) substituted by halogen, arbitrarily substituted phenyl by any, or form a 3~7-membered ring with N； R9 represents alkyl (1≦C≦7), alkyl (1≦C≦7) substituted by halogen, arbitrarily substituted phenyl； R10 and R11, being the same or different, represent alkyl (1≦C≦7), alkyl (1≦C≦7) substituted by halogen, arbitrarily substituted phenyl, or form a 3~7-membered ring with N； however, when Y is F, R3 and R4 will not be OH at the same time while R1 and R2 represent, hydrogen at the same time.) Futher, the above compound is reacted with a fluorinating reagent so as to prepare 18F-2-Fluoro-4-Borono-L-phenylalanine.本發明提供一種新穎之掌性4-硼苯丙胺酸(BPA)之衍生物、其製造方法、及使用該衍生物之18F標記化BPA(18F-2-氟-4-硼-L-苯丙胺酸；18F-BPA)之製造方法。本發明係調製下述式所示之化合物。此處，R表示BR3R4、BX3-、或BX3-M+(此處X表示鹵素，M+表示1價之單原子陽離子、多原子陽離子、或錯陽離子)；R1表示氫或保護基PG1；R2表示氫或保護基PG2；R3及R4分別表示OH，或與B(硼原子)共同形成作為B的保護基之環；Y表示鹵素、NO2、NH2、Sn(R6)3、N=N-NR7R8、OSO2R9、NR10R11或取代或無取代之苯基碘、取代或無取代之雜環基碘之任一者(此處，R6表示碳數1~7之烷基；R7及R8可相同或相異，表示氫、碳數1~7之烷基、被鹵素取代之碳數1~7之烷基、被任意取代之苯基，或與N共同形成具有3~7員之環構造；R9表示碳數1~7之烷基、被鹵素取代之碳數1~7之烷基、或被任意取代之苯基；R10及R11可相同或相異，表示碳數1~7之烷基、被鹵素取代
