Mild, Pd-catalyzed stannylation of radioiodination targets

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:25

Article

Pickett, Julie E.¹  Varadi, Andras¹  Palmer, Travis C.¹  Grinnell, Steven G.¹  Schrock, Joel M.¹  Pasternak, Gavril W.¹  Karimov, Rashad R.²  Majumdar, Susruta¹ 

[1] Mem Sloan Kettering Canc Ctr, Dept Neurol, Mol Pharmacol & Chem Program, New York, NY 10065 USA

[2] Mem Sloan Kettering Canc Ctr, Tri Inst Training Program Chem Biol, New York, NY 10065 USA

关键词: Stannylation;    Radioiodination;    Opioid;    Sigma receptor;    Radioligand binding;   

DOI  :  10.1016/j.bmcl.2015.02.055

来源: Elsevier

【 摘 要 】

Trialkylstannanes are versatile precursors for chemical transformations, including radiolabeling with a variety of halogens, particularly iodine. In the present work a convenient, Pd-mediated stannylation method is presented that can be performed in an open flask. The method is selective for aryl iodides allowing selective stannylations in the presence of other halogen atoms. The reaction conditions are mild, making the method compatible with chemically sensitive bioactive compounds. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

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