公开(公告)号：US20120184772A1

公开(公告)日：2012-07-19

申请号：US13497318

申请日：2010-09-28

申请人： Allan R. Bailey ,  Michelle M. Jones ,  Tino J. Caviggiola, III ,  Mills T. Kneller ,  Alexander N. Petrov ,  Michael A. Brown ,  Benjamin J. Costello

发明人： Allan R. Bailey ,  Michelle M. Jones ,  Tino J. Caviggiola, III ,  Mills T. Kneller ,  Alexander N. Petrov ,  Michael A. Brown ,  Benjamin J. Costello

IPC分类号： C07C231/12

CPC分类号： C07C231/12 ,  C07C237/46

摘要： The present disclosure is directed to a process for preparing an alkylated triiodo-substituted arylamide, such as iodixanol, the process comprising contacting a triiodo-substituted arylamide, such as 5-acetamido-N,N′-bis(2,3-dihydroxylpropyl)-2,4,6-triiodoisophthalamide, and an alkylating agent in the presence of a base and a mixed solvent system comprising a non-aqueous solvent and water, wherein the volume ratio of the non-aqueous solvent to water is greater than 1:1. The process advantageously enables the concentration of any impurities or undesirable byproduct from the reaction to be reduced, while increasing the yield of the desired reaction product.

摘要翻译： 本公开涉及制备烷基化三碘取代的芳基酰胺如碘克沙醇的方法，该方法包括使三碘取代的芳基酰胺如5-乙酰氨基-N，N'-双（2,3-二羟基丙基） -2,4,6-三碘间苯二酰胺和烷基化剂，在碱和包含非水溶剂和水的混合溶剂体系的存在下，其中非水溶剂与水的体积比大于1： 1。 该方法有利地使来自反应的任何杂质或不期望的副产物的浓度降低，同时增加所需反应产物的产率。

公开(公告)号：US20120184773A1

公开(公告)日：2012-07-19

申请号：US13497320

申请日：2010-09-28

申请人： Tino J. Caviggiola, III ,  Michelle M. Jones

发明人： Tino J. Caviggiola, III ,  Michelle M. Jones

IPC分类号： C07C231/12

CPC分类号： C07C231/12 ,  C07D265/36 ,  C07C237/46

摘要： The present disclosure generally relates to an improved process for alkylating a triiodo-substituted arylamide to form a compound suitable for use as an X-ray contrast agent. More particularly, the present disclosure is directed to such a process that limits the formation of fused bicyclic impurities, such as Impurity G, in the alkylation reaction mixture.

摘要翻译： 本公开内容通常涉及用于烷基化三碘取代的芳基酰胺以形成适合用作X射线造影剂的化合物的改进方法。 更具体地说，本公开涉及限制在烷基化反应混合物中稠合的双环杂质如杂质G的形成的方法。