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Specifications of Pyrrolo2,1-f1,2,4triazin-4-amine丨CAS 159326-68-8
|
Appearance |
White to brownish yellow solid |
|
Purity (HPLC) |
98.5% min. |
|
Identification |
The retention time of the test should correspond to the standard in purity |
|
Single impurity |
0.5% max. |
|
Total impurities |
1.0% max. |
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Water |
0.5% max. |
Overview
Pyrrolo2,1-f1,2,4triazin-4-amine丨CAS 159326-68-8 is a key nitrogen-rich heterocycle and an important pharmaceutical intermediate, especially in the development of antiviral agents.
Applications
1. Pharmaceutical Intermediate
Nucleoside Analogs Synthesis:
Pyrrolo2,1-f1,2,4triazin-4-amine丨CAS 159326-68-8 is a critical core intermediate in the synthesis of Remdesivir, a broad-spectrum antiviral used for COVID-19 and other RNA virus infections.
Antiviral Drug Development:
Its fused heterocyclic scaffold mimics purine bases (like adenine), making it highly valuable in nucleoside analog design for RNA polymerase inhibitors.
Potential Use in Oncology and Antibacterial Drugs:
The triazine scaffold has also been studied for applications in anticancer agents and enzyme inhibitors, particularly kinases.
2. Medicinal Chemistry Research
Widely used in structure–activity relationship (SAR) studies for designing purine bioisosteres or analogs with improved metabolic stability or altered receptor selectivity.
Serves as a base moiety for constructing small-molecule inhibitors in high-throughput drug screening.
3. Nucleoside and Nucleotide Chemistry
Acts as the heterocyclic base unit in the synthesis of C-nucleosides and modified RNA analogs, particularly where stability against enzymatic cleavage is desired.
4. Synthetic Organic Chemistry
Building block for the construction of more complex fused heterocycles. The electron-rich fused triazine-pyrrole system can undergo further substitutions, functionalizations, and ring modifications.
Benefits
1. Drug-Relevant Heterocycle
Structurally similar to biologically active purines, allowing effective mimicry of natural nucleobases, critical in antiviral and anticancer agents.
2. Versatile Reactivity
The presence of an exocyclic amine and electron-rich ring system offers multiple reactive sites for further derivatization and functional group modification.
3. High Value in Antiviral Therapeutics
As a known Remdesivir precursor, it plays a central role in the production of drugs that inhibit viral RNA-dependent RNA polymerases (RdRp), crucial for viral replication.
4. Stable and Scalable
Amenable to large-scale synthesis with manageable stability under standard storage and reaction conditions, important for industrial pharmaceutical manufacturing.
Conclusion
Pyrrolo2,1-f1,2,4triazin-4-amine丨CAS 159326-68-8 is a strategic intermediate in the synthesis of modern antiviral agents such as Remdesivir. Its fused nitrogen-rich heterocycle enables its use in developing nucleoside analogs, RNA therapeutics, and purine mimics, with broad applications in virology, oncology, and medicinal chemistry. Its importance is particularly pronounced in pharmaceutical manufacturing and drug discovery for viral diseases.
