Osimertinib represents a paradigm shift in targeted oncology, offering a well-characterized synthetic route that relies on a carefully orchestrated sequence of regioselective transformations. The synthesis proceeds through a convergent strategy: Friedel-Crafts pyrimidination constructs the indole-pyrimidine core, followed by SNAr coupling with the fluoro-nitroaniline moiety, subsequent amination with N,N,N'-trimethylethylenediamine, nitro reduction, and final acrylamide formation .
We offer the full series of key intermediates and related impurities to support your osimertinib research, development, and manufacturing programs.
|
Parameter |
Specification |
|
Product Name |
Osimertinib |
|
CAS Number |
1421373-65-0 |
|
Molecular Formula |
C₂₈H₃₃N₇O₂ |
|
Molecular Weight |
499.62 g/mol |
|
Appearance |
White to off-white crystalline powder |
|
Storage Condition |
2–8 °C, protected from light and moisture |
Definitive Third-Generation EGFR Inhibitor
Osimertinib is the standard-of-care treatment for EGFR-mutant NSCLC with T790M resistance, offering superior efficacy and CNS penetration compared to earlier-generation EGFR inhibitors. The acrylamide warhead enables covalent, irreversible binding with high selectivity for mutant EGFR over wild-type .
Well-Optimized, Convergent Synthetic Route
The commercial synthesis of osimertinib has been refined through convergent strategies, achieving overall yields of 40–77% with >99.8% purity from optimized patent routes . Key transformations include Friedel-Crafts pyrimidination, SNAr coupling, and controlled acrylamide formation.
Full Intermediate Supply Chain
Cosperpharm supplies the entire cascade of osimertinib intermediates—from the core fluoro-nitroaniline building block (4-fluoro-2-methoxy-5-nitroaniline) through advanced coupling intermediates. This enables flexible synthetic route development and risk mitigation in your manufacturing campaign.
High-Purity Reference Standards
Our impurity portfolio includes fully characterized Osimertinib Impurity 15 (4-fluoro-2-methoxy-6-nitroaniline) and Osimertinib N,N'-Dioxide with comprehensive analytical data (NMR, MS, HPLC) to support ANDA method validation and regulatory submissions .
Cosperpharm supplies Osimertinib API, the full series of key intermediates, and impurity reference standards with rigorous quality control and comprehensive documentation.
Whether you need R&D quantities for process development, reference standards for method validation, or bulk intermediates for commercial manufacturing, we deliver consistent quality with full batch traceability. Contact us today for a quote or to discuss your requirements.
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