Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.

Gao M; Kong D; Clearfield A; Zheng QH

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.

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Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.

机译：碳11和氟18标记的N-乙酰基-1-芳基-6,7-二甲氧基-1,2,3,4-四氢异喹啉衍生物的合成作为新的潜在PET AMPA受体配体。

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摘要

New carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed and synthesized as potential positron emission tomography AMPA (2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid) receptor ligands to image brain diseases. The single crystal structure of the most potent compound N-acetyl-1-(4'-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (5a) is first reported.

机译：设计并合成了新的碳11和氟18标记的N-乙酰基-1-芳基-6,7-二甲氧基-1,2,3,4-四氢异喹啉衍生物，作为潜在的正电子发射断层扫描AMPA（2-氨基-3- （3-羟基-5-甲基异恶唑-4-基）丙酸）受体配体对大脑疾病进行成像。最先报道最有效的化合物N-乙酰基-1-（4'-氯苯基）-6,7-二甲氧基-1,2,3,4-四氢异喹啉（5a）的单晶结构。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2006年第8期|共5页
作者
Gao M; Kong D; Clearfield A; Zheng QH;
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正文语种 eng
中图分类药学;生物化学;
关键词
Amides; Anticonvulsants; Isoquinolines; Receptors; AMPA; 酰胺类; 抗惊厥药; 异喹啉类; 受体; AMPA;

机译：Amides;Anticonvulsants;Isoquinolines;Receptors;AMPA;酰胺类;抗惊厥药;异喹啉类;受体;AMPA;

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1. Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands. [J] . Gao M, Kong D, Clearfield A, Bioorganic and Medicinal Chemistry Letters . 2006,第8期

机译：碳11和氟18标记的N-乙酰基-1-芳基-6,7-二甲氧基-1,2,3,4-四氢异喹啉衍生物的合成作为新的潜在PET AMPA受体配体。
2. Synthesis of new carbon-11 labeled cyclofenil derivatives for PET imaging of breast cancer estrogen receptors [J] . Gao M, Wang M, Mock BH, Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine . 2008,第4期

机译：新型碳11标记的环苯腈衍生物的合成，用于乳腺癌雌激素受体的PET显像
3. Fluorine-18 labeling of 6,7-disubstituted anilinoquinazoline derivatives for positron emission tomography (PET) imaging of tyrosine kinase receptors: synthesis of F-Iressa and related molecular probes [J] . Yann Seimbille, Michael E. Phelps, Johannes Czernin, Journal of Labelled Compounds and Radiopharmaceuticals . 2005,第11期

机译：6,7-二取代的苯胺基喹唑啉衍生物的氟18标记用于酪氨酸激酶受体的正电子发射断层扫描（PET）成像：F-Iressa和相关分子探针的合成
4. Two-step labeling allows analysis of neuronal AMPA-type glutamate receptors dynamics “beyond optical resolution limit” [C] . Kento Ojima, Mikiko Takato, Shigeki Kiyonaka 日本化学会春季年会講演予稿集 . 2018

机译：两步标记允许分析神经元AMPA型谷氨酸受体动态“超出光学分辨率限制”
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Synthesis Radiosynthesis and Biological Evaluation of Carbon-11 and Fluorine-18 Labeled Reboxetine Analogs: Potential Positron Emission Tomography Radioligands for in Vivo Imaging of the Norepinephrine Transporter [O] . Fanxing Zeng, Jiyoung Mun, Nachwa Jarkas, -1

机译：碳-11和氟-18标记的瑞波西汀类似物的合成放射合成和生物学评估：去甲肾上腺素转运蛋白体内成像的潜在正电子发射断层扫描放射配体
7. Synthesis, Radiosynthesis, and Biological Evaluation of Carbon-11 and Fluorine-18 (N-Fluoroalkyl) Labeled 2b-Carbomethoxy-3b-(4-(3-furyl)phenyl)tropanes and -nortropanes: Candidate Radioligands for in Vivo Imaging of the Serotonin Transporter with Positron Emission Tomography [O] . -1

机译：碳-11和氟-18（N-氟代烷基）标记的2b-碳甲氧基-3b-（4-（3-酪蛋白）苯基）的合成，可放射合成和生物学评价和 - - 中丙烷：体内成像的候选放射性配体血清素转运蛋白与正电子发射断层扫描
8. Synthesis of Carbon-11, Fluorine-18, and Nitrogen-13 Labeled Radiotracers for Biomedical Applications [R] . Fowler, J. S., Wolf, A. P. 1981

机译：用于生物医学应用的碳-11，氟-18和氮-13标记的放射性示踪剂的合成

Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.

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