Boc-Gly-Gly-NH2 | 61798-83-2

• 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: Boc-Gly-Gly-NH2
• 英文别名: N-(tert-Butoxycarbonyl)glycylglycinamide；tert-butyl N-[2-[(2-amino-2-oxoethyl)amino]-2-oxoethyl]carbamate
• CAS: 61798-83-2
• 化学式: C₉H₁₇N₃O₄
• mdl: MFCD24393368
• 分子量: 231.252
• InChiKey: WCMFSDIWPNHRHT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  16
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  111
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Boc-Gly-Gly-NH2 在 [双(三氟乙酰氧基)碘]苯 作用下， 以 水 、 乙腈 为溶剂， 反应 6.0h， 生成 [(Aminomethyl-carbamoyl)-methyl]-carbamic acid tert-butyl ester; compound with trifluoro-acetic acid
  参考文献：
  名称：

  Chorev, Michael; Gilon, Noemy; Roubini, Eli, Collection of Czechoslovak Chemical Communications, 1988, vol. 53, # 11A, p. 2519 - 2536

  摘要：

  DOI：
• 作为产物：
  描述：

  Boc-Gly-Gly-OEt 在 氨 作用下， 以 甲醇 为溶剂， 反应 12.0h， 以95.2%的产率得到Boc-Gly-Gly-NH2
  参考文献：
  名称：

  Chorev, Michael; Gilon, Noemy; Roubini, Eli, Collection of Czechoslovak Chemical Communications, 1988, vol. 53, # 11A, p. 2519 - 2536

  摘要：

  DOI：

文献信息

• [EN] METHOD FOR THE PRODUCTION OF 18F-LABELED ACTIVE ESTERS AND THEIR APPLICATION EXEMPLIFIED BY THE PREPARATION OF A PSMA-SPECIFIC PET-TRACER<br/>[FR] PROCÉDÉ DE PRODUCTION D'ESTERS ACTIFS MARQUÉS AU 18F ET LEUR APPLICATION ILLUSTRÉE PAR LA PRÉPARATION D'UN TRACEUR POUR PET SPÉCIFIQUE DE L'ANTIGÈNE MEMBRANAIRE SPÉCIFIQUE DE LA PROSTATE (PSMA)
  申请人：MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V

  公开号：WO2016030329A1

  公开（公告）日：2016-03-03

  Novel efficient, time-saving and reliable radiofluorination procedures for the production of 18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with 18F- are described. The active ester including [18F]F-Py-TFP and [18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.

  本文描述了一种高效、省时和可靠的放射性氟化程序，通过将相应的离子前体与18F-的亲核取代反应制备18F标记的活性酯。其中包括通过其中一种方法制备的[18F]F-Py-TFP和[18F]TFB的活性酯，用于制备PSMA特异性PET示踪剂，如[18F]DCFPyL。这些创新方法的关键优势是高效、制备时间短，且易于自动化。通过这些创新方法制备的至少一种PSMA特异性PET示踪剂的药物组合物，对于正电子发射断层扫描（PET）成像特别是前列腺肿瘤成像非常有用。
• [EN] PRODRUGS OF EXCITATORY AMINO ACIDS<br/>[FR] PROMEDICAMENTS D'ACIDES AMINES EXCITATEURS
  申请人：LILLY CO ELI

  公开号：WO2003104217A2

  公开（公告）日：2003-12-18

  This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.

  本发明涉及合成兴奋性氨基酸前药及其制备方法。本发明还涉及使用方法以及包含该化合物的药物组合物，用于治疗神经系统疾病和精神疾病。
• Method for the production of 18F-labeled PSMA-specific PET-tracers
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2993171A1

  公开（公告）日：2016-03-09

  Novel efficient, time-saving and reliable radiofluorination procedures for the production of 18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with 18F- are described. The active ester including [18F]F-Py-TFP and [18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.

  本文描述了一种高效、省时和可靠的放射性氟化程序，通过将相应的离子前体与18F进行亲核取代，制备18F标记的活性酯。其中包括通过这些方法制备的[18F]F-Py-TFP和[18F]TFB等活性酯，用于制备PSMA特异性PET示踪剂，如[18F]DCFPyL。这些创新方法的关键优势是效率高、制备时间短和易于自动化。含有至少一种通过创新方法制备的PSMA特异性PET示踪剂的制药组合物，对于正电子发射断层扫描（PET）成像特别是前列腺肿瘤成像非常有用。
• ANTIBODY-DRUG CONJUGATE PRODUCED BY BINDING THROUGH LINKER HAVING HYDROPHILIC STRUCTURE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2910573A1

  公开（公告）日：2015-08-26

  As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH-(CH2)n1-La-Lb-Lc- or -L1-L2-LP- wherein the antibody is connected to the terminal of L1, the antitumor compound is connected to the terminal of Lc or LP, and any one or two or more of linkers of L1, L2, and LP has a hydrophilic structure.

  作为一种抗肿瘤效果和安全性俱佳的抗肿瘤药物，本发明提供了一种抗体-药物共轭物，其中下式（I）表示的抗肿瘤化合物通过具有下式表示的结构的连接体与抗体共轭：-L1-L2-LP-NH-(CH2)n1-La-Lb-Lc-或-L1-L2-LP-，其中抗体连接到 L1 的末端，抗肿瘤化合物连接到 Lc 或 LP 的末端，并且 L1、L2 和 LP 中的任意一个或两个或多个连接体具有亲水结构。
• Engelfried,C. et al., Liebigs Annalen der Chemie, 1979, p. 973 - 985
  作者：Engelfried,C. et al.

  DOI：——

  日期：——