CAS: 60166-93-0; (S)-N1,N3-Bis(1,3-Dihydroxypropan-2-yl)-5-(2-Hydroxypropanamido)-2,4,6-Triiodoisophthalamide

上下游产品

CAS号60166-91-8 S-(-)-5-[[2-(ac... | CAS号534-03-2 丝氨醇 | CAS号35453-19-1 5-氨基-2,4,6-三碘间苯二甲酸

在 水,Sodium Hydroxide体系中,用 N,N-二甲基乙酰胺 作为反应溶剂,以992 G的收率获得产物碘帕醇
参考文献: Process For The Preparation Of Iopamidol[fr] Procédé De Préparation D'Iopamidol
标题: Process For The Preparation Of Iopamidol[fr] Procédé De Préparation D'Iopamidol
摘要:本发明公开了一种制备式iopamidol(II)的过程,包括以下步骤:A)将化合物(i)与酰化剂(S)-2-(乙酰氧基)丙酰氯在反应介质中反应,其中x为or2或r3,R2和r3为c1-C6线性或支链烷基,C3-C6环烷基,C6芳基,可选地取代为甲基,乙基,正丙基,异丙基,正丁基,仲丁基,叔丁基和苯基,以提供化合物(i)的乙酰氧衍生物;b)将步骤a)中间体与ph为0至7的水溶液水解,通过加入水或稀释的碱性溶液如氢氧化钠或氢氧化钾,释放含硼保护基的羟基,获得化合物(II)的n-(S)-2-(乙酰氧基)丙酰衍生物;c)碱性水解以恢复(S)-2-(羟基)丙酰基团并获得iopamidol(II),并可从步骤b)中获得的溶液中可选地回收硼衍生物.含硼保护基具有多功能性,高效性和可回收性.提供了一锅法合成,无需中间体分离,减少了回收和再利用的溶剂,显著提高了产率,从成本效益和环保意识方面具有显著优势.

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-5817861-A
优先权日:1996-03-29
标题 :Process for the preparation of an intermediate useful in the synthesis of iodinated contrast media
发明人：VILLA MARCO; NARDI ANTONIO; PAIOCCHI MAURIZIO
权利人:BRACCO INT BV
摘要:A process for the preparation of (S)-N,N'-bis 2-hydroxy-1-(hydroxymethyl)ethyl!-5-(2-acetoxy-propionylamino)-2,4,6-triiodo-isophthalamide, an intermediate useful for the synthesis of iopamidol, by reaction between L-5-(2-acetoxy-propionylamino)-2,4,6-triiiodoisophthaloyl dichloride and 2-amino-1 ,3-propanediol in N-methylpyrrolidone and in the presence of a base, is described.

专利号:US-9549995-B2
优先权日:2012-03-26
标 题:Efficient synthesis of ethylenedicysteine-sugar conjugates for imaging and therapy
发明人：YANG DAVID J; YU DONG-FANG
权利人:UNIV TEXAS
摘要:Novel methods of synthesis of ethylenedicysteine-sugar conjugates and therapeutic and diagnostic applications of such conjugates are disclosed. Methods of synthesizing these conjugates in high purity are also presented as using starting materials such as thiazolidine carboxylic acid. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these conjugates prepared herein, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:WO-2024256322-A1
优先权日:2023-06-13
标题 :Synthesis of non-ionic radiographic contrast agents by means of reactive extrusion
发明人：LATTUADA LUCIANO; SEBASTIANO ROBERTO; LEONARDI GABRIELLA; CRAVOTTO GIANCARLO; BARGE ALESSANDRO; BUCCIOL FABIO
权利人:BRACCO IMAGING SPA; MILANO POLITECNICO
摘要:The present invention relates to the industrial preparation of non-ionic X-ray contrast agents. In particular, it relates to a process for the synthesis of lopamidol using a reactive extrusion process in continuous which enable an efficient conversion of the relevant key intermediates, preferably in the absence of any solvent. The invention further relates to the preparation of radiographic X-rays contrast agents or key intermediates thereof by exploiting the technology of reactive extrusion.

专利号:WO-2025073833-A1
优先权日:2023-10-04
标 题:Optimized process for the preparation of iopamidol
发明人：BUONSANTI FEDERICA; MAZZON ROBERTA; FRETTA ROBERTA
权利人:BRACCO IMAGING SPA
摘要:The present invention relates to the field of organic chemistry, in particular to the synthesis of iodinated contrast agents. More in particular, the invention relates to a sustainable process for the synthesis of iopamidol which allows to improve the purity profile of the product and avoids the use of potentially hazardous reagents and solvents.

专利号:US-12006540-B2
优先权日:2015-09-28
标题:Synthesis of novel disulfide linker based nucleotides as reversible terminators for DNA sequencing by synthesis
发明人：JU JINGYUE; LI XIAOXU; CHEN XIN; LI ZENGMIN; KUMAR SHIV; SHI SHUNDI; GUO CHENG; REN JIANYI; HSIEH MIN-KANG; CHIEN MINCHEN; TAO CHUANJUAN; ERTURK ECE; KALACHIKOV SERGEY; RUSSO JAMES J
权利人:UNIV COLUMBIA
摘要:Disclosed herein, inter alia, are compounds, compositions, and methods of use thereof in the sequencing of a nucleic acid.