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Apremilast Intermediate (CAS 253168-94-4), chemically identified as 1-(3-Ethoxy-4-methoxy-phenyl)-2-methanesulfonyl-ethylamine, a pivotal aminosulfone building block. In pharmaceutical landscape, this intermediate serves as the essential chiral precursor for the synthesis of Apremilast (Otezla), a blockbuster oral therapy. Aminosulfone Intermediate intermediate contains the core phenethylamine scaffold and the methylsulfonyl moiety that are vital for the drug's high affinity toward its target enzyme. For CDMOs and Bulk Manufacturers, achieving the correct stereochemistry-specifically the (S)-enantiomer (CAS 608141-42-0)- (CQA) that determines the efficacy of the final API. We are a globally established CAS 253168-94-4 supplier and various pharmaceutical APIs, intermediates, excipients, finished formulations, and dosages from sourcing, r&d to manufacturing scaling through comprehensive regulatory documentation (CoA), compliances, traceability, and consistent worldwide supply capabilities, ensuring reliable lead times and quality assurance across all grades.
Apremilast Intermediate (CAS 253168-94-4), chemically identified as 1-(3-Ethoxy-4-methoxy-phenyl)-2-methanesulfonyl-ethylamine, a pivotal aminosulfone building block. In pharmaceutical landscape, this intermediate serves as the essential chiral precursor for the synthesis of Apremilast (Otezla), a blockbuster oral therapy. Aminosulfone Intermediate intermediate contains the core phenethylamine scaffold and the methylsulfonyl moiety that are vital for the drug's high affinity toward its target enzyme. For CDMOs and Bulk Manufacturers, achieving the correct stereochemistry-specifically the (S)-enantiomer (CAS 608141-42-0)- (CQA) that determines the efficacy of the final API. We are a globally ...
Chemical Properties & Specifications
Acute Tox. 4 (66.7%), Acute Tox. 4 (66.7%), Skin Irrit. 2 (33.3%), Eye Irrit. 2 (33.3%), Acute Tox. 4 (66.7%)
P261, P264, P264+P265, P270, P271, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P317, P321, P330, P332+P317, P337+P317, P362+P364, and P501
Late-stage condensation with 3-acetamidophthalic anhydride to form Apremilast
Catalytic asymmetric hydrogenation routes to bypass expensive chiral resolution steps
In regulatory environments-Tracked as "process-related impurity" under ICH Q3A/Q3B guidelines
Validate HPLC and LC-MS methods for drug substance purity testing by QC laboratories
Chemical "node" for developing next-generation PDE4 inhibitors for respiratory conditions (Asthma/COPD) and neuroinflammatory research
As a PDE4 inhibitor, it works by increasing intracellular levels of cyclic adenosine monophosphate (cAMP). This e levation indirectly modulates the production of numerous inflammatory mediators
Down-regulates: Pro-inflammatory cytokines like TNF-a, IL-23, and Interferon-gamma (IFN-Y)
Up-regulates: Anti-inflammatory cytokines like IL-10
Only the (S)-enantiomer of the aminosulfone yields the pharmacologically active form of Apremilast. Utilizing the pure (S)-isomer (CAS 608141-42-0) during the early stages of synthesis prevents the need for costly chiral resolution at the final API stage, significantly improving overall yield and atom economy.
This intermediate (CAS 253168-94-4) is often listed as Impurity H in European Pharmacopoeia (EP) monographs. This means that for manufacturers of the final drug, monitoring the residual levels of this aminosulfone is a regulatory requirement to ensure the safety and purity of the finished Otezla tablets.
Chiral Resolution: Synthesizing the racemic form and resolving it with chiral acids.
Asymmetric Hydrogenation: Chiral catalyst to directly synthesize the (S)-form from a corresponding keto-sulfone or enamine precursor. This second route is increasingly favored for high-volume B2B production due to its higher efficiency.
Should be stored in a cool, dry place (preferably 2-8°C) under an inert atmosphere (Nitrogen). While the sulfone group is stable, the primary amine moiety is sensitive to atmospheric carbon dioxide and moisture, which can lead to degradation over time.
