2-(3-Methylbut-2-en-2-yl)-1,3-benzothiazole | 1029129-50-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: 2-(3-Methylbut-2-en-2-yl)-1,3-benzothiazole
• 英文别名: 2-(3-methylbut-2-en-2-yl)-1,3-benzothiazole
• CAS: 1029129-50-7
• 化学式: C₁₂H₁₃NS
• 分子量: 203.308
• InChiKey: DMSSRXQURKJAKE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  苯并噻唑 、 2-溴-3-甲基-2-丁烯 在 PdCl(C₃H₅)(dppb) caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 20.0h， 以58%的产率得到2-(3-Methylbut-2-en-2-yl)-1,3-benzothiazole
  参考文献：
  名称：

  Alkenyl bromides: useful coupling partners for the palladium-catalysed coupling with heteroaromatics via a C–H bond activation

  摘要：

  Alkenyl bromides were found to be useful reactants for the palladium-catalysed direct C-H activation/functionalisation reaction of heteroaromatics such as benzoxazole or benzothiazole. Moderate to good yields of coupling products were obtained using both alpha- and P-substituted alkenyl bromides or even the trisubstituted alkenyl bromide 2-bromo-3-methylbut-2-ene. This reaction is environmentally attractive as it provides only HX associated to the base as a by-product. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2008.03.020

文献信息

• Bifunctional molecules for degradation of EGFR and methods of use
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US11161842B2

  公开（公告）日：2021-11-02

  The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.

  本申请提供了式 (I) 的双官能化合物： 其可作为表皮生长因子受体和/或其突变体的蛋白质降解诱导分子。本申请还描述了通过使用双功能化合物靶向降解表皮生长因子受体和/或其突变体的方法，该双功能化合物将泛素配体结合分子与能够与表皮生长因子受体和/或其突变体结合的配体连接起来，可用于治疗受表皮生长因子受体或其突变体调节的疾病。
• BIFUNCTIONAL MOLECULES FOR DEGRADATION OF EGFR AND METHODS OF USE
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20200102298A1

  公开（公告）日：2020-04-02

  The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.
• Alkenyl bromides: useful coupling partners for the palladium-catalysed coupling with heteroaromatics via a C–H bond activation
  作者：Aditya L. Gottumukkala、Fazia Derridj、Safia Djebbar、Henri Doucet

  DOI：10.1016/j.tetlet.2008.03.020

  日期：2008.4

  Alkenyl bromides were found to be useful reactants for the palladium-catalysed direct C-H activation/functionalisation reaction of heteroaromatics such as benzoxazole or benzothiazole. Moderate to good yields of coupling products were obtained using both alpha- and P-substituted alkenyl bromides or even the trisubstituted alkenyl bromide 2-bromo-3-methylbut-2-ene. This reaction is environmentally attractive as it provides only HX associated to the base as a by-product. (c) 2008 Elsevier Ltd. All rights reserved.