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公开(公告)号：EP3112340B1
公开(公告)日：2020-07-15
申请号：EP15754420.6
申请日：2015-01-28
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2.发明公开METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO, AND PRECURSOR OF 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO 审中-公开用于生产4硼-L-苯丙氨酸进口它18F原子和4硼-L-苯丙氨酸PRE进口它18F-ATOM
公开(公告)号：EP3112340A1
公开(公告)日：2017-01-04
申请号：EP15754420.6
申请日：2015-01-28
发明人： TAKENAKA, Hiroshi , OHTA, Yoichiro , TAGUCHI, Yusuke , UEDA, Sayuri , ISHINO, Yuko , YOSHIKAWA, Tomohiro , NAKASHIMA, Hideki , UEHARA, Kohki , KIRIHATA, Mitsunori
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).
摘要翻译： 本发明的目的是提供：一种新的制造方法18 F-标记的4硼 - 苯丙氨酸（BPA）; 和18的前体F-标记的BPA。 18 F-标记的BPA可以通过制备由式（1）表示的化合物和使用该化合物来制备。 在该式中，R 1表示溴基于碘基，氟基，diazaborinane衍生物，BX3-或BX3-M +（worin X表示卤素原子;和M + darstellt一价单原子阳离子，多原子阳离子或复杂 阳离子）。
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3.发明公开PRODUCTION METHOD FOR 2-FLUORO-4-BORONO-L-PHENYLALANINE, AND PRECURSOR OF 2-FLUORO-4-BORONO-L-PHENYLALANINE 审中-公开2-氟-4-硼-l-苯基白氨酸的生产方法和2-氟-4-硼-l-苯基白氨酸的前体
公开(公告)号：EP3085687A1
公开(公告)日：2016-10-26
申请号：EP14872762.1
申请日：2014-12-16
发明人： TAKENAKA, Hiroshi , OHTA, Yoichiro , TAGUCHI, Yusuke , UEDA, Sayuri , ISHINO, Yuko , YOSHIKAWA, Tomohiro , NAKASHIMA, Hideki , UEHARA, Kohki , KIRIHATA, Mitsunori
IPC分类号： C07C229/36 , C07C251/24 , C07C271/22 , C07F5/02 , C07F7/22 , C07B59/00
CPC分类号： C07F5/027 , C07C229/36 , C07C251/24 , C07C271/22 , Y02P20/55
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.)
摘要翻译： 本发明涉及制备由下式表示的化合物。 （式中，R 1表示Br基，碘基，Cl基，NO 2基或NH 2基，R 2表示卤素基，NO 2基，NH 2基，Sn（R 6）3，N = N-NR7R8，OSO2R9，NR10R11，苯基碘鎓，杂环基碘，硼酸或硼酸酯; R30代表保护基PG1; R40或R50代表氢，保护基PG2或C6H5（C6H5）C = N ，其中NR40R50在一起）。
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公开(公告)号：EP2907818B1
公开(公告)日：2018-08-15
申请号：EP13846717.0
申请日：2013-10-08
发明人： TAKENAKA, Hiroshi , OHTA, Yoichiro , TAGUCHI, Yusuke , UEDA, Sayuri , ISHINO, Yuko , NAKASHIMA, Hideki , UEHARA, Kohki , KIRIHATA, Mitsunori
IPC分类号： C07F5/04 , C07C229/36 , C07F5/02 , C07B59/00 , C07C271/22 , C07C251/24
CPC分类号： C07F5/025 , C07B59/001 , C07C229/08 , C07C229/36 , C07C251/24 , C07C271/22 , C07F5/027 , C07F5/04 , Y02P20/55
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.
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5.发明公开CHIRAL 4-BORONOPHENYLALANINE (BPA) DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING 18F-LABELED BPA USING SAID DERIVATIVE 审中-公开手性4-硼 - 苯丙氨酸（BPA）及其制造衍生物和方法以及制造方法18 F-标记的BPA BY所述衍生物
公开(公告)号：EP2907818A1
公开(公告)日：2015-08-19
申请号：EP13846717.0
申请日：2013-10-08
发明人： TAKENAKA, Hiroshi , OHTA, Yoichiro , TAGUCHI, Yusuke , UEDA, Sayuri , ISHINO, Yuko , NAKASHIMA, Hideki , UEHARA, Kohki , KIRIHATA, Mitsunori
IPC分类号： C07F5/04 , C07C229/36 , C07F7/22 , C07B59/00
CPC分类号： C07F5/025 , C07B59/001 , C07C229/08 , C07C229/36 , C07C251/24 , C07C271/22 , C07F5/027 , C07F5/04 , Y02P20/55
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。
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