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2. 发明授权

US06420568B1 Process for making 1,3-disubstituted-4-oxocyclic ureas 有权
标题翻译： 1,3-二取代-4-氧杂环脲的制备方法
公开(公告)号：US06420568B1
公开(公告)日：2002-07-16
申请号：US09674228
申请日：2000-10-27
申请人： Patricia Ann Matson , Michael Selden Godlewski
发明人： Patricia Ann Matson , Michael Selden Godlewski
IPC分类号： C07D40512
CPC分类号： C07D405/12
摘要： A process for making 1,3-disubstituted-4-oxocyclic ureas of general formula (I): wherein R1, R2, and R3 are independently selected from the group consisting of nil, Cl, F, Br, NH2, NO2, COOH, CH3SO2NH, SO3H, OH, alkoxy, alkyl, alkoxycarbon hydroxyalkyl, carboxyalkyl, and acyloxy; R4 is selected from the group consisting of a substituted or unsubstituted alkyl, alkenyl alkynyl, alkylacyl, and heteroalkyl; and A is a substituted or unsubstituted, saturated or unsaturated, straight-chain or branched alkyl or alkenyl amino group comprised of 1-7 carbon atoms; or A is a substituted or unsubstituted, saturated or unsaturated heterocycle having 5, 6, or 7 members containing at least one nitrogen, and R4 is attached to this nitrogen; wherein said 1,3-disubstituted tuted-4-oxocyclic urea is made without isolation of intermediates and comprising the steps: (Ia) reacting a l-substituted-4-oxocyclic urea with a carbon chain containing at least two leaving groups in the presence of a mild base and a solvent to form an adduct containing at least one leaving group, and (Ib) condensing the adduct with an amine to form a 1,3-disubstituted-4-oxocyclic urea, and (II) recovering said 1-3-disubstituted-4-oxocyclic urea, are disclosed. This method is particularly preferred for making [[[5-(4-Chlorophenyl)2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl)-2,4-imidazolidinedione.
摘要翻译：制备通式（I）的1,3-二取代-4-氧代环脲的方法：其中R 1，R 2和R 3独立地选自n，Cl，F，Br，NH 2，NO 2，COOH， CH3SO2NH，SO3H，OH，烷氧基，烷基，烷氧基碳羟烷基，羧基烷基和酰氧基; R4选自取代或未取代的烷基，烯基炔基，烷基酰基和杂烷基; 并且A是由1-7个碳原子组成的取代或未取代的饱和或不饱和的直链或支链烷基或烯基氨基; 或A是具有5,6或7个含有至少一个氮的成员的取代或未取代的饱和或不饱和杂环，并且R 4连接到该氮上; 其中所述1,3-二取代的哌啶-4-氧杂环脲在不分离中间体的情况下制备，并且包括以下步骤：（Ia）使1-取代-4-氧代环脲与含有至少两个离去基团的碳链在存在下反应的温和碱和溶剂以形成含有至少一个离去基团的加合物，和（Ib）将加合物与胺缩合以形成1,3-二取代-4-氧代环脲，和（II）回收所述1- 3-二取代-4-氧代环脲。该方法对于制备[[[（5-氯苯基）-2-呋喃基]亚甲基]氨基] -3- [4-（4-甲基-1-哌嗪基）丁基）-2,4-咪唑烷二酮是特别优选的。

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