(2-vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester | 1094070-78-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (2-vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester
• 英文别名: tert-butyl N-(2-ethenyl-1,3-thiazol-5-yl)carbamate
• CAS: 1094070-78-6
• 化学式: C₁₀H₁₄N₂O₂S
• 分子量: 226.299
• InChiKey: ZMEFZKPZWCCIFC-UHFFFAOYSA-N

物化性质

• 密度：
  1.209±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  79.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (2-vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester 在 三乙酰氧基硼氢化钠 2,6-二甲基吡啶 、 sodium periodate 、 四氧化锇 、 溶剂黄146 作用下， 以 1,4-二氧六环 、 水 、 1,2-二氯乙烷 、 异丙醇 为溶剂， 反应 7.0h， 生成 (2-Morpholin-4-ylmethyl-thiazol-5-yl)-carbamic acid tert-butyl ester
  参考文献：
  名称：

  WO2008/156614

  摘要：

  公开号：
• 作为产物：
  描述：

  2-溴噻唑-5-氨基甲酸叔丁基酯 、 三丁基乙烯基锡 在 四(三苯基膦)钯 作用下， 以 1,4-二氧六环 为溶剂， 生成 (2-vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors

  摘要：

  Our continued effort toward the development of the imidazo[1,2-a] pyrazine scaffold as Aurora kinase inhibitors is described. Bioisosteric approach was applied to optimize the 8-position of the core. Several new potent Aurora A/B dual inhibitors, such as 25k and 25l, were identified. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.10.008
• 作为试剂：
  描述：

  2-溴噻唑-5-氨基甲酸叔丁基酯 、 三丁基乙烯基锡 、 2,6-二叔丁基-4-甲基苯酚 在 四(三苯基膦)钯 (2-vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester 、 乙酸乙酯 、 crude material 作用下， 以 1,4-二氧六环 为溶剂， 反应 12.0h， 以to yield (2-Vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester (solid) 1.1 g (54%)的产率得到(2-vinyl-thiazol-5-yl)-carbamic acid tert-butyl ester
  参考文献：
  名称：

  ANTI-MITOTIC AGENT AND AURORA KINASE INHIBITOR COMBINATION AS ANTI-CANCER TREATMENT

  摘要：

  本发明涉及一种通过预先使用抗有丝分裂剂，然后再使用至少一种极化素激酶抑制剂来治疗癌症的方法。详细说明了在本发明治疗中有用的抗有丝分裂剂和极化素激酶抑制剂。

  公开号：

  US20100249030A1

文献信息

• IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS
  申请人：Schering Corporation

  公开号：EP2170892A2

  公开（公告）日：2010-04-07
• [EN] IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS<br/>[FR] IMIDAZOPYRAZINES COMME INHIBITEURS DE LA PROTÉINE KINASE
  申请人：SCHERING CORP

  公开号：WO2008156614A2

  公开（公告）日：2008-12-24

  [EN] In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions.
  [FR] Dans ses nombreux modes de réalisation, la présente invention porte sur une nouvelle classe de composés imidazopyrazine comme inhibiteurs de protéine et/ou d'Aurora kinases, sur des procédés de préparation de ces composés, sur des compositions pharmaceutiques comprenant un ou plusieurs de ces composés, sur des procédés de préparation de formulations pharmaceutiques comprenant un ou plusieurs de ces composés et sur des procédés de traitement, de prévention, d'inhibition ou d'amélioration d'une ou plusieurs maladies associées aux protéines ou Aurora kinases à l'aide de ces composés et de ces compositions pharmaceutiques.
• [EN] ANTI-MITOTIC AGENT AND AURORA KINASE INHIBITOR COMBINATION AS ANTI-CANCER TREATMENT<br/>[FR] COMBINAISON D'AGENT ANTIMITOTIQUE ET D'INHIBITEUR DE L'AURORA KINASE COMME TRAITEMENT ANTI-CANCER
  申请人：SCHERING CORP

  公开号：WO2009017701A2

  公开（公告）日：2009-02-05

  The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.
• [EN] NOVEL STEROID PAYLOADS, STEROID LINKERS, ADCs CONTAINING AND USE THEREOF<br/>[FR] NOUVELLE CHARGE UTILE DE STÉROÏDE, LIEURS DE STÉROÏDES, CAM LES CONTENANT ET UTILISATION ASSOCIÉE
  申请人：[en]IMMUNEXT, INC.

  公开号：WO2022150637A1

  公开（公告）日：2022-07-14

  The invention provides novel glucocorticosteroids, glucocorticosteroid-linkers and antibody drug conjugates (ADC's) comprising an antibody or antibody fragment which binds to an antigen expressed on immune cells, optionally an antigen expressed on human immune cells. In some instances the ADCs comprise an anti-human VISTA (V-region Immunoglobulin-containing Suppressor of T cell Activation(1)) antibody or anti-VISTA antigen-binding antibody fragment which binds to VISTA expressing cells at physiologic pH having a short serum half-life (≈ 24-72 or 24-48 or 12-24 hours or less in a human VISTA knock-in rodent or ((≈ 1-3.5 days or less in a human or non-human primate). In some instances these ADCs have a rapid onset of action and are potent for prolonged duration as they are very effectively internalized by immune cells in large amounts where they are cleaved releasing large amounts of active steroid payload. The invention also relates to the use of such ADCs and novel steroids for the treatment of autoimmune, allergic and inflammatory conditions. The invention further relates to methods for reducing the adverse side effects and/or enhancing the efficacy of glucocorticoid receptor agonists by using such ADCs to selectively deliver these anti-inflammatory agents to target immune cells, such as monocytes, neutrophils, B cells, T cells, Tregs, eosinophils, NK cells, macrophages, myeloid cells, et al., and particularly myeloid cells, thereby reducing potential toxicity to non-target cells.