公开(公告)号：US08487126B2

公开(公告)日：2013-07-16

申请号：US13499724

申请日：2010-09-22

申请人： Hisao Nemoto ,  Tomoyuki Kawamura ,  Kenji Yatsuzuka ,  Masaki Kamiya

发明人： Hisao Nemoto ,  Tomoyuki Kawamura ,  Kenji Yatsuzuka ,  Masaki Kamiya

IPC分类号： C07C69/34 ,  C07C229/00

CPC分类号： C07D207/452 ,  C07C227/16 ,  C07C233/47 ,  C07C271/08 ,  C07C271/12 ,  C07C229/30

摘要： The objective of the present invention is to provide a process for simple and efficient preparation of an intermediate compound to synthesize a gadolinium complex having a substituent for improving a retention property in blood time and specificity to an intended organ. The objective of the present invention is also to provide an intermediate compound produced by the said production process. The process for preparation of the diethylenetriaminepentaacetic acid derivative (I): wherein R1 to R5 are independently C1-6 alkyl groups; comprising the steps of: reacting a diethylenetriaminepentaacetic acid pentaester with a halogenated ally compound in an aprotic solvent; removing the excess halogenated ally compound (III); and reacting a reaction product of the diethylenetriaminepentaacetic acid pentaester and the halogenated ally compound with a base in a solvent.

摘要翻译： 本发明的目的是提供简单有效地制备中间体化合物以合成具有取代基的钆络合物的方法，以提高血液时间的保留性和对预期器官的特异性。 本发明的目的还在于提供通过所述生产方法制备的中间体化合物。 制备二亚乙基三胺五乙酸衍生物（I）的方法：其中R 1至R 5独立地为C 1-6烷基; 包括以下步骤：使二亚乙基三胺五乙酸五酯与卤化烯化合物在非质子溶剂中反应; 除去过量的卤代烯化合物（III）; 并使二亚乙基三胺五乙酸五酯与卤代烯化合物的反应产物与碱在溶剂中反应。

公开(公告)号：US20120203027A1

公开(公告)日：2012-08-09

申请号：US13499724

申请日：2010-09-22

申请人： Hisao Nemoto ,  Tomoyuki Kawamura ,  Kenji Yatsuzuka ,  Masaki Kamiya

发明人： Hisao Nemoto ,  Tomoyuki Kawamura ,  Kenji Yatsuzuka ,  Masaki Kamiya

IPC分类号： C07C227/16 ,  C07C229/30

CPC分类号： C07D207/452 ,  C07C227/16 ,  C07C233/47 ,  C07C271/08 ,  C07C271/12 ,  C07C229/30

摘要： The objective of the present invention is to provide a process for simple and efficient preparation of an intermediate compound to synthesize a gadolinium complex having a substituent for improving a retention property in blood time and specificity to an intended organ. The objective of the present invention is also to provide an intermediate compound produced by the said production process. The process for preparation of the diethylenetriaminepentaacetic acid derivative (I): wherein R1 to R5 are independently C1-6 alkyl groups; comprising the steps of: reacting a diethylenetriaminepentaacetic acid pentaester with a halogenated ally compound in an aprotic solvent; removing the excess halogenated ally compound (III); and reacting a reaction product of the diethylenetriaminepentaacetic acid pentaester and the halogenated ally compound with a base in a solvent.

摘要翻译： 本发明的目的是提供简单有效地制备中间体化合物以合成具有取代基的钆络合物的方法，以提高血液时间的保留性和对预期器官的特异性。 本发明的目的还在于提供通过所述生产方法制备的中间体化合物。 制备二亚乙基三胺五乙酸衍生物（I）的方法：其中R 1至R 5独立地为C 1-6烷基; 包括以下步骤：使二亚乙基三胺五乙酸五酯与卤化烯化合物在非质子溶剂中反应; 除去过量的卤代烯化合物（III）; 并使二亚乙基三胺五乙酸五酯与卤代烯化合物的反应产物与碱在溶剂中反应。