• 1. Acenaphthenic hopanoids, a novel series of aromatised
  Teresita Carrillo-Hernández,Philippe Schaeffer,Pierre Albrecht Chem. Commun., 2001, 1976-1977
• 2. An artificial enzyme cascade amplification strategy for highly sensitive and specific detection of breast cancer-derived exosomes?
  Huiying Xu,Lu Zheng,Yu Zhou,Bang-Ce Ye Analyst, 2021,146, 5542-5549
• 3. An artificial photosynthesis system comprising a covalent triazine framework as an electron relay facilitator for photochemical carbon dioxide reduction?
  Siquan Zhang,Shengyao Wang,Liping Guo,Hao Chen,Bien Tan,Shangbin Jin J. Mater. Chem. C, 2020,8, 192-200
• 4. An amorphous lanthanum–iridium solid solution with an open structure for efficient water splitting?
  Wei Sun,Chenglong Ma,Xinlong Tian,Jianjun Liao,Ji Yang,Chengjun Ge,Weiwei Huang J. Mater. Chem. A, 2020,8, 12518-12525
• 5. An apparatus for testing water by measurement of its electrical conductivity
  Analyst, 1912,37, 538-543

• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Indoles and derivatives Indoles

Recent Advances in the Application of 4-Bromo-1-(triisopropylsilyl)-1H-indole (CAS: 412048-44-3) in Chemical Biology and Pharmaceutical Research

The compound 4-Bromo-1-(triisopropylsilyl)-1H-indole (CAS: 412048-44-3) has emerged as a pivotal intermediate in the synthesis of complex bioactive molecules, particularly in the fields of medicinal chemistry and chemical biology. Recent studies have highlighted its utility in the construction of indole-based scaffolds, which are prevalent in numerous pharmaceuticals and biologically active compounds. This research brief synthesizes the latest findings on the applications, synthetic methodologies, and biological relevance of this compound.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the efficacy of 4-Bromo-1-(triisopropylsilyl)-1H-indole as a precursor in the synthesis of novel kinase inhibitors. The triisopropylsilyl (TIPS) protecting group was found to enhance the stability of the indole nucleus during multi-step reactions, enabling the efficient introduction of bromine at the 4-position for subsequent cross-coupling reactions. This approach has been instrumental in the development of targeted therapies for oncology applications.

In the realm of chemical biology, researchers have leveraged the unique reactivity of 4-Bromo-1-(triisopropylsilyl)-1H-indole to develop fluorescent probes for protein labeling. A recent ACS Chemical Biology publication (2024) detailed its use in creating environment-sensitive fluorophores through palladium-catalyzed coupling reactions. These probes have shown exceptional utility in live-cell imaging studies, particularly for tracking protein-protein interactions in real time.

The pharmaceutical industry has shown increasing interest in this compound as evidenced by several patent applications filed in 2023-2024. One notable application involves its use as a key intermediate in the synthesis of serotonin receptor modulators, with potential applications in neurological disorders. The bromine atom at the 4-position allows for precise functionalization through modern cross-coupling techniques, while the TIPS group provides necessary protection during synthetic transformations.

Recent advancements in synthetic methodology have expanded the utility of 412048-44-3. A 2024 Organic Letters report described a novel continuous flow process for its preparation, achieving higher yields (85-90%) and reduced reaction times compared to traditional batch methods. This development addresses previous challenges in scaling up production while maintaining high purity standards required for pharmaceutical applications.

From a biological perspective, derivatives synthesized from 4-Bromo-1-(triisopropylsilyl)-1H-indole have demonstrated promising activity in preliminary screening against various cancer cell lines. Molecular modeling studies suggest that the indole scaffold, when properly functionalized, can effectively interact with the ATP-binding sites of several protein kinases. Current research is focusing on optimizing these interactions to improve selectivity and reduce off-target effects.

In conclusion, 4-Bromo-1-(triisopropylsilyl)-1H-indole (412048-44-3) continues to be a versatile building block in medicinal chemistry and chemical biology research. Its unique combination of reactivity and stability makes it particularly valuable for the development of novel therapeutic agents and research tools. Future research directions likely include exploration of its applications in PROTAC development and as a precursor for more complex heterocyclic systems.

• 148249-36-9(3-Bromo-1-(triisopropylsilyl)indole)
• 331432-91-8(1H-Indole,5-bromo-1-[(1,1-dimethylethyl)dimethylsilyl]-)
• 123191-00-4(1H-Indole,1-[tris(1-methylethyl)silyl]-)
• 184637-11-4(6-Bromo-1-(tert-butyldimethylsilyl)indole)
• 128564-66-9(5-bromo-1-[tris(propan-2-yl)silyl]-1H-indole)
• 1015609-27-4(6-Bromo-1-(triisopropylsilyl)-1h-pyrrolo3,2-bpyridine)
• 918148-84-2(2-Bromo-1-[tri(propan-2-yl)silyl]-1H-indole)
• 193694-04-1(4-Bromo-1-(tert-butyldimethylsilyl)indole)
• 153942-69-9(1H-Indole, 3-bromo-1-[(1,1-dimethylethyl)dimethylsilyl]-)
• 184636-93-9(1H-Indole, 3,6-dibromo-1-[(1,1-dimethylethyl)dimethylsilyl]-)