公开(公告)号：US09126961B2

公开(公告)日：2015-09-08

申请号：US13848877

申请日：2013-03-22

申请人： GE HEALTHCARE LIMITED ,  GE HEALTHCARE AS

发明人： Anthony Eamon Storey ,  Clare Louise Jones ,  Denis Raymond Christophe Bouvet ,  Nicholas Lasbistes ,  Steven Michael Fairway ,  Lorenzo Williams ,  Alexander Mark Gibson ,  Robert James Nairne ,  Farhad Karimi ,  Bengt Langstrom

IPC分类号： C07D277/66

CPC分类号： A61K51/0453 ,  B01J19/24 ,  B01J2219/24 ,  C07D277/66 ,  Y02P20/55

摘要： The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.

摘要翻译： 本发明涉及制备式（I）化合物的方法：R1选自C 1-6烷基，C 2-6烯基和C 2-6炔基; 其包括：（i）与氟化物，适当的[18 F]氟化物反应，相应的式（II）化合物：其中R 2选自氢，C 1-10烷基，C 1-10卤代烷基，C 6-14芳基，C 6-14芳烷基， （CH 2 CH 2 O）q -CH 3，其中q是1至10的整数; R1如式（I）化合物所定义; R3是离去基团。 还要求具有式（II）的某些新型前体和含有这些前体的放射性药物试剂盒。

公开(公告)号：US09468694B2

公开(公告)日：2016-10-18

申请号：US14809497

申请日：2015-07-27

申请人： GE Healthcare Limited ,  GE Healthcare AS

发明人： Anthony Eamon Storey ,  Clare Louise Jones ,  Denis Raymond Christophe Bouvet ,  Nicolas Lasbistes ,  Steven Michael Fairway ,  Lorenzo Williams ,  Alexander Mark Gibson ,  Robert James Nairne ,  Farhad Karimi ,  Bengt Langstrom

IPC分类号： B01J19/24 ,  C07D277/66 ,  A61K51/04

CPC分类号： A61K51/0453 ,  B01J19/24 ,  B01J2219/24 ,  C07D277/66 ,  Y02P20/55

摘要： The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.

公开(公告)号：US20150328344A1

公开(公告)日：2015-11-19

申请号：US14809497

申请日：2015-07-27

申请人： GE Healthcare Limited ,  GE Healthcare AS

发明人： Anthony Eamon Storey ,  Clare Louise Jones ,  Denis Raymond Christophe Bouvet ,  Nicolas Lasbistes ,  Steven Michael Fairway ,  Lorenzo Williams ,  Alexander Mark Gibson ,  Robert James Nairne ,  Farhad Karimi ,  Bengt Langstrom

IPC分类号： A61K51/04 ,  B01J19/24 ,  C07D277/66

CPC分类号： A61K51/0453 ,  B01J19/24 ,  B01J2219/24 ,  C07D277/66 ,  Y02P20/55

摘要： The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.

摘要翻译： 本发明涉及制备式（I）化合物的方法：R1选自C 1-6烷基，C 2-6烯基和C 2-6炔基; 其包括：（i）与氟化物，适当的[18 F]氟化物反应，相应的式（II）化合物：其中R 2选自氢，C 1-10烷基，C 1-10卤代烷基，C 6-14芳基，C 6-14芳烷基， （CH 2 CH 2 O）q -CH 3，其中q是1至10的整数; R1如式（I）化合物所定义; R3是离去基团。 还要求具有式（II）的某些新型前体和含有这些前体的放射性药物试剂盒。

公开(公告)号：US20220009919A1

公开(公告)日：2022-01-13

申请号：US17174155

申请日：2021-02-11

申请人： GE Healthcare Limited

发明人： Lorenzo Williams ,  Gunnar Keilen ,  Jarle Andre Haugan

IPC分类号： C07D451/02 ,  C07F7/00 ,  C07F7/22

摘要： The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123I-labelled radiopharmaceutical DaTSCAN™ (123I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.

公开(公告)号：US20160376265A1

公开(公告)日：2016-12-29

申请号：US15199108

申请日：2016-06-30

申请人： GE Healthcare Limited

发明人： Lorenzo Williams ,  Gunnar Keilen ,  Jarle Andre Haugan

IPC分类号： C07D451/02 ,  C07F7/00

CPC分类号： C07D451/02 ,  C07F7/00 ,  C07F7/2208

摘要： The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123I-labelled radiopharmaceutical DaTSCAN™ (123I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.

摘要翻译： 本发明涉及使用氟烷基碘改进的合成N-单氟烷基托烷。 本发明还提供了使用这种方法来制备非放射性托烷中间体FP-CIT，并且其随后转化为123I标记的放射性药物DaTSCAN TM（123I-氟烷）。 还提供了在本发明的烷基化方法中使用氟代烷基碘。