CAS: 3718-88-5; 3-Iodobenzylamine Hydrochloride

该化合物是一种有机化合物,其特点是附于苯环的氨基(-NH2)组,该组在元体位置上也有碘替代物.该化合物一般是白色至白晶状固体,由于存在盐状,可溶解于水中,与自由基相比,盐状提高了其溶性.碘原子有助于其独特的再活动,使其在各种合成应用中,特别是在医药化学和有机合成中发挥作用.该化合物可能展示生物活动,其衍生物往往被探索用于潜在的药物用途.与许多阿明斯一样,该化合物可能具有基本特性,并可以参与各种化学反应,包括核循环替代和组合反应.适当的处理和储存与许多化学物质一样,对于确保安全和稳定至关重要.

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CAS号60076-09-7 间碘氯苄 | CAS号152918-18-8 匹利诺生 | CAS号163152-30-5 (2R,3S,4R,5R)-2... | CAS号163042-96-4 氯-IB-MECA | CAS号263351-43-5 3-碘苄基氨基甲酸叔丁酯 | CAS号72158-53-3 9H-Purin-6-amin... | CAS号80663-95-2 间碘苯胍硫酸盐 | CAS号80663-96-3 3-IODOBENZYL-GU...

合成工艺路线路线简述

    间碘氯苄置于盐酸,乌洛托品体系中,化学反应生成 3-碘苄胺盐酸盐
    参考文献:替代作用.14.水-有机溶剂混合物中的离解常数异常:苄基铵离子和相关系统
    标题:替代作用.14.水-有机溶剂混合物中的离解常数异常:苄基铵离子和相关系统
    摘要:给出了对于苄基铵,苄基二烷基铵和(2-苯乙基)铵离子的各种水-有机溶剂混合物中的热力学解离常数.与hammett方程(方程式1)的偏差与对羧酸观测到的偏差相似,但符号相反.包含疏水常数π的扩展hammett方程(等式3)产生了非常好的相关性.举例说明了派生的次级正常sigma值.
    DOI:10.1002/recl.19921110103

    海关参考信息

    专利信息


    专利号:US-9102698-B2
    优先权日:2007-03-14
    标 题:Process for the synthesis of IB-MECA
    发明人:BRUZINSKI PAUL; LIU XUEJUN; GIBB CAMERON; HERNANDEZ-ABAD PEDRO E
    权利人:BRUZINSKI PAUL; LIU XUEJUN; GIBB CAMERON; HERNANDEZ-ABAD PEDRO E; CAN FITE BIOPHARMA LTD
    摘要:The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.

    专利号:US-8076499-B2
    优先权日:2009-08-13
    标 题 :Method for preparing precursor of radioactive 3-iodobenzylguanidine
    发明人:LIU SHOW-WEN; LIN CHENG-HSIEN; LIN TSYH-LANG; HSU CHENG-FANG
    权利人:LIU SHOW-WEN; LIN CHENG-HSIEN; LIN TSYH-LANG; HSU CHENG-FANG; ATOMIC ENERGY COUNCIL
    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 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 [*l]MIBG.

    专利号:US-5565185-A
    优先权日:1994-07-20
    标 题 :Process for the preparation of radiolabeled meta-halobenzylguanidine
    发明人:HUNTER DUNCAN H; GOEL ALOK; FLANAGAN RICHARD J
    权利人:MERCK FROSST CANADA INC
    摘要:The present invention provides a no-carrier-added synthesis of radiolabeled meta-halobenzylguanidine by halodestannylation which comprises reacting a meta-trialkylstannylbenzylguanidine with a source of radionuclide of a halogen. The present invention also provides meta-trialkylstannylbenzylguanidine as intermediates in the afore-mentioned process.

    专利号:US-2010087636-A1
    优先权日:2007-03-14
    标题:Process for the synthesis of ib-meca

    专利号:WO-2008111082-A1
    优先权日:2007-03-14
    标题 :Process for the synthesis of ib-meca

    专利号:DK-2137202-T3
    优先权日:2007-03-14
    标题:PROCEDURE FOR SYNTHESIS OF IB-MECA
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    主要参考文献

    参考标题:A Mild And General One-Pot Synthesis Of Densely Functionalized Diaryliodonium Salts
    作者:Linlin Qin,Bao Hu,Kiel D. Neumann,Ethan J. Linstad,Katelyenn Mccauley,Jordan Veness,Jayson J. Kempinger,Stephen G. Dimagno |发布日期:2015.9
    摘要:Diaryliodonium Salts Are Powerful And Widely Used Arylating Agents In Organic Chemistry. Here We Report A Scalable, Synthesis Of Densely Functionalized Diaryliodonium Salts From Aryl Iodides Under Mild Conditions. This Two-Step, One-Pot Process Has Remarkable Functional Group Tolerance, Is Compatible With Commonly Employed Acid-Labile Protective Group Strategies, Avoids Heavy Metal And Transition Metal

    合成参考文献


    参考文献:10.1007/s11094-020-02178-y
    摘要:Kapustyan AV, Buryak AA, Boiko VM. Development and Validation of an Analytical Method for Meta-Iodobenzylguanidine Sulfate Radiolabeled with 127I and 131I. Pharmaceutical Chemistry Journal. 2020 May 16;54(2):201–7. doi: 10.1007/s11094-020-02178-y.
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