2-Iodotyrosine | 70055-93-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-Iodotyrosine
• 英文别名: (2S)-2-amino-3-(4-hydroxy-2-iodophenyl)propanoic acid
• CAS: 70055-93-5
• 化学式: C₉H₁₀INO₃
• 分子量: 307.08
• InChiKey: BMBZSHPNHVPCNG-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  83.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  溴甲基甲基醚 、 3-碘苯甲醚 、 2-Iodotyrosine 在 乙酸乙酯 、 Sodium sulfate-III 、 silica gel 作用下， 以 溶剂黄146 、 水 为溶剂， 反应 48.0h， 以to yield 1-bromomethyl-2-iodo-4-methoxybenzene (20) as a white solid (4.59 g, 45%)的产率得到1-(bromomethyl)-2-iodo-4-methoxybenzene
  参考文献：
  名称：

  Nucleophilic fluorination of aromatic compounds

  摘要：

  取代了电子给予和电子吸引基团的碘苯衍生物可用作芳香族亲核取代反应的前体。亚碘基团（IO2）被亲核性氟离子区域特异性地取代，从而提供相应的氟代芳基衍生物。无载体添加的[F-18]氟离子，可以从无水[F-18]（F/Kryptofix，[F-18]CsF或季铵氟化物（例如，Me4NF，Et4NF，n-Bu4NF，（PhCH2）4NF）中获得，它们仅取代这些衍生物中的亚碘基团，并提供高比活度的F-18标记的氟代芳基类似物。苯并噻唑类似物和6-碘-L-多巴衍生物的碘衍生物已合成为前体，并用于制备无载体添加的[F-18]氟代苯并噻唑以及6-[F-18]氟-L-多巴。

  公开号：

  US08674101B2

文献信息

• [EN] PROTEASOME INHIBITING ß-LACTAM PRODRUGS USEFUL FOR THE TREATMENT OF CANCER AND NEURODEGENERATIVE DISORDERS<br/>[FR] PROMÉDICAMENTS À BASE DE SS-LACTAME INHIBITEURS DU PROTÉASOME UTILES POUR LE TRAITEMENT DU CANCER ET DE TROUBLES NEURODÉGÉNÉRATIFS
  申请人：VITA API

  公开号：WO2018115497A1

  公开（公告）日：2018-06-28

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明通常涉及抑制蛋白酶体的β-内酰胺化合物，用于治疗癌症和神经退行性疾病。该发明还提供了所述化合物的药物组合物和延长释放配方，以及利用所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医疗用途。
• Diagnostic and therapeutic agents
  申请人：Taube Seija

  公开号：US20070258899A1

  公开（公告）日：2007-11-08

  Tumor targeting units are disclosed which have a peptide sequence C y —Y—G-F—X—W-G-Z-C yy (SEQ ID NO: 25), or a pharmaceutically or physiologically acceptable salt thereof. Tumor targeting agents are also disclosed having at least one targeting unit, directly or indirectly coupled to at least one effector unit. Diagnostic or pharmaceutical compositions having at least one targeting unit or at least one targeting agent, and targeting units or targeting agents for the preparation of a medicament for the treatment of cancer related diseases (including cancer), especially for the treatment of colon/colorectal cancer or its metastases are also disclosed.

  揭示了具有肽序列Cy—Y—G-F—X—W-G-Z-Cyy（序列ID编号：25）或其药学或生理上可接受的盐的肿瘤靶向单元。还披露了具有至少一个靶向单元的肿瘤靶向剂，直接或间接地偶联至至少一个效应单元。还披露了具有至少一个靶向单元或至少一个靶向剂的诊断或药物组合物，以及用于制备治疗癌症相关疾病（包括癌症）的药物的靶向单元或靶向剂，特别是用于治疗结肠/结直肠癌或其转移的靶向单元或靶向剂。
• NUCLEOPHILIC FLUORINATION OF AROMATIC COMPOUNDS
  申请人：Satyamurthy Nagichettiar

  公开号：US20110178302A1

  公开（公告）日：2011-07-21

  Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO 2 ) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me 4 NF, Et 4 NF, n-Bu 4 NF, (PhCH 2 ) 4 NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.

  取代了电子给予基团和电子吸引基团的碘苯衍生物在芳香族亲核取代反应中被用作前体。亚碘酰基团(IO2)被亲核氟以区域特异性取代，提供相应的氟芳基衍生物。无载体添加的[F-18]氟离子源自无水[F-18](F/Kryptofix、[F-18]CsF或季铵氟化物(例如Me4NF、Et4NF、n-Bu4NF、(PhCH2)4NF))，只取代这些衍生物中的亚碘酰基团，并提供高比活度的F-18标记的氟芳基类似物。苯并噻唑类似物和6-碘-L-多巴衍生物的亚碘衍生物已被合成为前体，并用于制备无载体添加的[F-18]氟苯并噻唑和6-[F-18]氟-L-多巴。
• PROTEASOME INHIBITING SS-LACTAM PRODRUGS USEFUL FOR THE TREATMENT OF CANCER AND NEURODEGENERATIVE DISORDERS
  申请人：VITA API

  公开号：EP3339291A1

  公开（公告）日：2018-06-27

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明一般涉及用于治疗癌症和神经退行性疾病的蛋白酶体抑制β-内酰胺化合物。本发明还提供了所述化合物的药物组合物和缓释制剂，以及所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医学用途。
• Proteasome inhibiting β-lactam prodrugs useful for the treatment of cancer and neurodegenerative disorders
  申请人：Vita Api

  公开号：US11053249B2

  公开（公告）日：2021-07-06

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明一般涉及用于治疗癌症和神经退行性疾病的蛋白酶体抑制β-内酰胺化合物。本发明还提供了所述化合物的药物组合物和缓释制剂，以及所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医学用途。