Synthesis of a mGluR5 antagonist using [~(11)Clcopper(I) cyanide

William B. Mathews; James A Monn; Hayden T. Ravert; Daniel P.Holt; Darryle D. Schoepp; Robert F. Dannals

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Synthesis of a mGluR5 antagonist using [~(11)Clcopper(I) cyanide

机译：使用[〜（11）Clcopper（I）氰化物合成mGluR5拮抗剂

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摘要

5-(2-Phenylethynyl)pyridine-3-[~(11)C]carbonitrile ([~(11)C]LY2232645), a metabotropic glutamate 5 receptor (mGluR5) antagonist, was synthesized by a no-carrier-added nucleophilic halogen displacement with [~(11)C]copper(I) cyanide. The average radio-chemical yield was 2.5%, and the average specific activity was 1365mCi/mumol at end-of-synthesis. The total time of synthesis, purification, and formulation was 26min

机译：通过无载体亲核试剂合成了代谢型谷氨酸5受体拮抗剂5-（2-苯基乙炔基）吡啶-3- [〜（11）C]腈（[〜（11）C] LY2232645）用[〜（11）C]氰化铜（I）取代卤素。在合成结束时，平均放射化学产率为2.5％，平均比活为1365mCi / mumol。合成，纯化和配制的总时间为26分钟

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来源
《Journal of Labelled Compounds and Radiopharmaceuticals》 |2006年第9期|共6页
作者
William B. Mathews; James A Monn; Hayden T. Ravert; Daniel P.Holt; Darryle D. Schoepp; Robert F. Dannals;
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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
~(11)C; copper cyanide; glutamate; mGluR5; PET;

机译：〜（11）C;氰化铜;谷氨酸盐;mGluR5;PET;

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1. Synthesis of a mGluR5 antagonist using [~(11)Clcopper(I) cyanide [J] . William B. Mathews, James A Monn, Hayden T. Ravert, Journal of Labelled Compounds and Radiopharmaceuticals . 2006,第9期

机译：使用[〜（11）Clcopper（I）氰化物合成mGluR5拮抗剂
2. Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain [J] . SonM.-H., KimJ.Y., LimE.J., Bioorganic and Medicinal Chemistry Letters . 2013,第5期

机译：2-（芳基乙炔基）喹啉衍生物作为MgluR5拮抗剂治疗神经性疼痛的合成和生物学评价
3. Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain [J] . SonM.-H., KimJ.Y., LimE.J., Bioorganic and Medicinal Chemistry Letters . 2013,第5期

机译：mGluR5拮抗剂2-（芳乙炔基）喹啉衍生物的合成及生物学评价
4. ~(99m)Tc LABELLED PEPTIDE F11: A NEW POTENTIAL α_vβ_3 INTEGRIN ANTAGONIST FOR SCINTIGRAPHIC DETECTION OF TUMOURS [C] . A. PERERA, A. PRATS, A. HERNANDEZ, Trends in Radiopharmaceuticals(ISTR-2005) . 2007

机译：〜（99m）Tc标记的肽F11：用于肿瘤影像学检测的新型潜力α_vβ_3整合剂
5. Hypercoordinate silicon compounds in organic synthesis: Improved methods for the synthesis of aryl(trialkoxy)silane derivatives; and trimethylsilyl cyanide as a cyanide source for nucleophilic substitution. [D] . Manoso, Amy Slover. 2004

机译：有机合成中的超配位硅化合物：合成芳基（三烷氧基）硅烷衍生物的改进方法；三甲基甲硅烷基氰化物作为亲核取代的氰化物来源。
6. Synthesis and SAR of an mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold [O] . Sameer Sharma, Alice L. Rodriguez, P. Jeffrey Conn, -1

机译：mGluR5变构部分拮抗剂前导物的合成与合成孔径雷达：药理学的意外调节对5-（苯基乙炔基）嘧啶骨架有轻微的结构修饰
7. Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold [O] . Sameer Sharma, Alice L. Rodriguez, P. Jeffrey Conn, 2008

机译：MGLUR5变构偏拮抗剂铅的合成和SAR：对5-（苯基乙炔基）嘧啶支架具有轻微结构改性的药理意外调制

Synthesis of a mGluR5 antagonist using [~(11)Clcopper(I) cyanide

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