(R,E)-TCO-NHS Ester

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (R,E)-TCO-NHS Ester
• 英文别名: [(1R,2E)-cyclooct-2-en-1-yl] (2,5-dioxopyrrolidin-1-yl) carbonate
• 化学式: C₁₃H₁₇NO₅
• 分子量: 267.28
• InChiKey: IXECMLNTLPRCJD-RWCYGVJQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  72.9
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• [EN] CHEMICALLY CLEAVABLE GROUP<br/>[FR] GROUPE CLIVABLE PAR VOIE CHIMIQUE
  申请人：TAGWORKS PHARMACEUTICALS B V

  公开号：WO2014081303A1

  公开（公告）日：2014-05-30

  Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactice components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine.

  本文揭示了逆电子需求Diels-Alder反应的反应性组分用于体外化学掩蔽和解除掩蔽。这可以应用于复杂的化学反应中，特别是在生物分子合成中，例如在固相支持上。反应性组分包括双烯，特别是反式环辛二烯，和二烯，特别是四氮唑。
• [EN] TETRAZINES FOR HIGH CLICK RELEASE SPEED AND YIELD<br/>[FR] TÉTRAZINES POUR UNE VITESSE ET UN RENDEMENT DE LIBÉRATION DE CHIMIE CLIC ÉLEVÉS
  申请人：TAGWORKS PHARMACEUTICALS B V

  公开号：WO2020256544A1

  公开（公告）日：2020-12-24

  Disclosed herein are tetrazines substituted with groups that result in a high click conjugation yield and high click release yields. In some of several other aspects, the invention relates to combinations and kits comprising said tetrazines and a dienophile, preferably a trans-cyclooctene. In another aspect, the compounds, combinations, and kits are for use as a medicament.

  本文揭示了用于高点击共轭产量和高点击释放产量的基团替代的四唑类化合物。在其他几个方面，本发明涉及包括所述四唑类化合物和双亲核烯的组合和试剂盒，其中双亲核烯优选为反-环辛烯。在另一个方面，这些化合物、组合和试剂盒可用作药物。
• [EN] AGENTS FOR CLEAVING LABELS FROM BIOMOLECULES IN VIVO<br/>[FR] AGENTS PERMETTANT DE CLIVER IN VIVO DES MARQUEURS LIÉS À DES BIOMOLÉCULES
  申请人：TAGWORKS PHARMACEUTICALS B V

  公开号：WO2020256545A1

  公开（公告）日：2020-12-24

  Disclosed herein are compounds comprising trans-cyclooctene moieties, combinations, and kits that can be used to more quickly remove radionuclides from a subject, preferably a human being. Said compounds, combinations and kits can also be used to increase the tumor-to-blood ratio, or to more rapidly and/or conveniently achieve such an increase, of a label in targeted imaging or targeted radiotherapy in a subject, preferably a human being.

  本文所披露的化合物包括顺-环辛烯基团，组合物和套装，可用于更快地从受试者（最好是人）中清除放射性核素。所述化合物、组合物和套装还可用于增加靶向成像或靶向放射治疗中标记物的肿瘤/血液比率，或更快地和/或更方便地实现这种增加，适用于受试者（最好是人）。
• CHEMICALLY CLEAVABLE GROUP
  申请人：TAGWORKS PHARMACEUTICALS B.V.

  公开号：US20150344514A1

  公开（公告）日：2015-12-03

  Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactive components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine.

  本发明揭示了在体外使用反电子需求Diels-Alder反应的反应组分进行化学遮蔽和解除遮蔽的方法。这可以应用于复杂的化学反应中，特别是在生物分子的合成中，例如在固体支持体上。反应组分是二烯丙烯，特别是反式-环辛烯，和二烯，特别是四唑。
• Chemically cleavable group
  申请人：Tagworks Pharmaceuticals B.V.

  公开号：US10927139B2

  公开（公告）日：2021-02-23

  Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactive components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine.

  本发明公开了利用反电子需求 Diels Alder 反应的反应组分进行体外化学掩蔽和解除掩蔽的方法。这可用于复杂的化学反应，特别是生物大分子的合成，例如在固体支持物上的合成。反应组分是亲二烯（尤其是反式环辛烯）和二烯（尤其是四嗪）。