CAS: 59782-87-5; 6-Chloro-5-Iodonicotinic Acid

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📜5-甲基-3-氨基-2-氯吡啶置于盐酸,Potassium Permanganate,Sodium Nitrite体系中,用 水 作为反应溶剂,化学反应 6.75H,反应生成 6-氯-5-碘烟酸
参考文献:Synthesis,Radiolabeling And Preliminary In Vivo Evaluation Of Multimodal Radiotracers For Pet Imaging And Targeted Radionuclide Therapy Of Pigmented Melanoma
标题:Synthesis,Radiolabeling And Preliminary In Vivo Evaluation Of Multimodal Radiotracers For Pet Imaging And Targeted Radionuclide Therapy Of Pigmented Melanoma
摘要:Melanin Pigment Represents An Attractive Target To Address Specific Treatment To Melanoma Cells,Such As Cytotoxic Radionuclides. However,Less Than Half Of The Patients Have Pigmented Metastases. Hence,Specific Marker Is Required To Stratify This Patient Population Before Proceeding With Melanin-Targeted Radionuclide Therapy. In Such A Context,We Developed Fluorinated Analogues Of A Previously Studied Melanin-Targeting Ligand,N-(2-Diethylaminoethyl)-6-Iodoquinoxaline-2-Carboxamide (Icf01012). These Latter Can Be Labeled Either With F-18 Or I-131/i-125 For Positron Emission Tomography Imaging (Melanin-Positive Patient Selection) And Targeted Radionuclide Therapy Purposes. Here We Describe The Syntheses,Radiosyntheses And Preclinical Evaluations On Melanoma-Bearing Mice Model Of Several Iodo-And Fluoro(Hetero)Aromatic Derivatives Of The Icf01012 Scaffold. After Preliminary Planar Gamma Scintigraphic And Positron Emission Tomography Imaging Evaluations,[i-125]-And [f-18]-N-[2-(Diethylamino)Ethyl]-4-Fluoro-3-Iodobenzamides ([i-125]4,[f-18]4) Were Found To Be Chemically And Biologically Stable With Quite Similar Tumor Uptakes At 1 H P.I. (9.7 +/-2.6% Id/g And 6.8 +/-1.9% Id/g,Respectively). (C) 2015 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2015.01.034