公开(公告)号：US20100234611A1

公开(公告)日：2010-09-16

申请号：US12063470

申请日：2006-08-11

申请人： 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

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： C07D277/66 ,  G21C1/01

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：US08410312B2

公开(公告)日：2013-04-02

申请号：US12063470

申请日：2006-08-11

申请人： 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

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： C07C211/46

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。