公开(公告)号：US20100056804A1

公开(公告)日：2010-03-04

申请号：US12203214

申请日：2008-09-03

申请人： Show-Wen LIU ,  Tsyh-Lang Lin ,  Cheng-Fang Hsu ,  Cheng-Hsien Lin ,  Tsai-Yueh Luo ,  Lie-Hang Shen ,  Hwa-Jan Chen

发明人： Show-Wen LIU ,  Tsyh-Lang Lin ,  Cheng-Fang Hsu ,  Cheng-Hsien Lin ,  Tsai-Yueh Luo ,  Lie-Hang Shen ,  Hwa-Jan Chen

IPC分类号： C07D207/30

CPC分类号： C07D207/46 ,  Y02P20/55

摘要： A compound containing carboxylate ester and N2S2 ligand bi-functional groups and a manufacturing method thereof are disclosed. The S in the N2S2 ligand of the compound containing carboxylate ester and N2S2 ligand bi-functional groups includes a protective group so as to avoid to be oxidized and easy storage. In a complex reaction, the protective group is automatically released As to the active carboxylate ester, it is for reacting with compounds having amino groups such as amines, amino acids, peptides, or protein etc while the N2S2 ligand is for bonding with technetium or rhenium so as to form neutral complex. The compound containing carboxylate ester and N2S2 ligand bi-functional groups is applied to radiopharmaceuticals such as contrast agents for tissues and target agents.

摘要翻译： 公开了含有羧酸酯和N 2 S 2配位体双官能团的化合物及其制备方法。 含有羧酸酯和N2S2配位体双官能团的化合物的N2S2配体中的S包括保护基，以避免被氧化并容易储存。 在复杂的反应中，保护基被自动释放对于活性羧酸酯，它是与具有氨基的化合物如胺，氨基酸，肽或蛋白质等反应，而N2S2配体与锝或铼键合 从而形成中性复合物。 含有羧酸酯和N 2 S 2配位体双功能基团的化合物被应用于放射性药物，例如用于组织和靶标的造影剂。

公开(公告)号：US20110040119A1

公开(公告)日：2011-02-17

申请号：US12540448

申请日：2009-08-13

申请人： Show-Wen LIU ,  Cheng-Hsien Lin ,  Tsyh-Lang Lin ,  Cheng-Fang Hsu

发明人： Show-Wen LIU ,  Cheng-Hsien Lin ,  Tsyh-Lang Lin ,  Cheng-Fang Hsu

IPC分类号： C07C271/20

CPC分类号： C07C277/08 ,  C07B2200/05 ,  C07C279/06

摘要： A method for preparing a precursor of radioactive 3-iodobenzylguanidine-N,N′-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The MSnBG is a precursor of [*I]MIBG that is used as radioactive imaging agents and antineoplastic drugs. The method includes following steps. Firstly, obtain 3-iodobenzylguanidine bicarbonate by an addition reaction between 3-iodobenzylamine hydrochloride and cyanamide. Use di-tert-butyl dicarbonate as a protecting agent for NH group and convert 3-iodobenzylguanidine bicarbonate into N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine. At last, under catalysis of bis(triphenylphosphine) palladium dichloride, obtain a final product MSnBG by a substitution reaction between N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine and bis(tri-n-butyltin). MSnBG is used in no-carrier-added synthesis of [*I]MIBG. The [*I]MIBG obtained by this method has better effect on neuroblastoma treatment than that obtained by conventional, carrier-added method.

摘要翻译： 揭示了制备放射性3-碘苄基胍-N，N'-双（叔丁氧基羰基）-3-（三正丁基锡）苄基胍）（MSnBG）的前体的方法。 MSnBG是用作放射性成像剂和抗肿瘤药物的[* I] MIBG的前体。 该方法包括以下步骤。 首先，通过3-碘苄胺盐酸盐和氨腈之间的加成反应获得3-碘苄基胍碳酸氢盐。 使用二碳酸二叔丁酯作为NH基团的保护剂，并将3-碘苄基胍碳酸氢盐转化成N，N'-双（叔丁氧基羰基）-N-（3-碘苄基）胍。 最后，在双（三苯基膦）二氯化钯的催化下，通过N，N'-双（叔丁氧基羰基）-N-（3-碘苄基）胍与双（三正丁基）二氯化钯的取代反应得到最终产物MSnBG， 丁基锡）。 MSnBG用于[* I] MIBG的无载体添加合成。 通过该方法获得的[* I] MIBG对于神经母细胞瘤治疗比通过常规的载体添加方法获得的效果更好。