摘要:
The purpose of the present invention is to provide: a novel method for producing 18 F-labeled 4-boronophenylalanine (BPA) ; and a precursor of 18 F-labeled BPA. 18 F-labeled BPA can be produced by preparing a compound represented by formula (1) and using the compound. In the formula, R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3- or BX3-M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).
摘要:
The present invention involves preparing compounds represented by the formula. (In the formula: R 1 represents a Br group, an iodine group, a Cl group, an NO 2 group, or an NH 2 group; R 2 represents a halogen group, an NO 2 group, an NH 2 group, Sn(R 6 ) 3 , N=N-NR 7 R 8 , OSO 2 R 9 , N R 10 R 11 , phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R 30 represents a protective group PG 1 ; R 40 or R 50 represent hydrogen, a protective group PG 2 , or C 6 H 5 (C 6 H 5 )C=N, wherein NR 40 R 50 are together.)
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.
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.
摘要翻译:本发明提供:一种新型的手性4-硼 - 苯丙氨酸(BPA)衍生物; 用于生产衍生物的方法; 以及用于制造18 F-2-氟-4-羟硼基-L-苯丙氨酸的方法(18 F标记的BPA; 18F-BPA)使用所述衍生物。 由式(1)表示的化合物制备。 在该式中,R darstellt BR 3 R 4,BX 3 - 或BX 3 - M +(worin X表示卤原子,M + darstellt一价单原子阳离子,多原子阳离子或阳离子络合物); R 1表示氢原子或保护基PG1; R 2表示氢原子或保护基PG2; R 3和R 4独立地表示OH,或R 3,R 4和B一起形成环也用作保护基团; 和Y代表卤原子,NO 2,NH 2,锡(R 6)3,N = N-NR 7 R 8,OSO 2 R 9,NR 10 R 11,substituiertem奥德unsubstituiertem phenyliodo基或substituiertem奥德unsubstituiertem 杂环碘基团。 的化合物与氟化试剂反应以制备18 F标记的BPA。