Arformoterol tartrate

Arformoterol tartrate is the active pharmaceutical ingredient (API) in the FDA-approved nebulizer solution Brovana® (Sunovion Pharmaceuticals), representing the pharmacologically active isomer of the racemic formoterol. As a potent β₂-agonist, Arformoterol tartrate stimulates intracellular adenylate cyclase, leading to bronchial smooth muscle relaxation with a rapid onset and a prolonged duration due to its high lipophilicity and retention in the lipid bilayer. Unlike racemic formoterol, Arformoterol tartrate contains only the eutomer, which is associated with a lower theoretical risk of non-specific cardiac effects mediated by the (S,S)-distomer. Cosperpharm manufactures Arformoterol tartrate under full ICH Q7 GMP conditions, providing generic pharmaceutical companies with a high-purity API that meets all compendial requirements and can be directly used in the formulation of nebulized solutions.

Product Parameters

Synthetic Route

Using 1-(4-benzyleoxy-3-nitrophenyl)-2-bromoacetone 187 as the starting material, its carbonyl group was reduced via an asymmetric reduction reaction to yield the R-configured brominated alcohol 186 with optical purity of 94%. Under the action of Adams catalyst, the nitro group of the brominated alcohol was catalytically hydrogenated to form an amino group, which subsequently reacted with formic acid to produce the amide compound 184. On the other hand, 1-(4-methoxyphenyl)propane-2-one underwent a reduction amination reaction with benzylamine, and the R-configured N-benzyl-1-(4-methoxyphenyl)propane-2-amine 183 was obtained via (S)-mandelic acid hydrolysis with Chemicalbook, achieving optical purity of 99.5%. In the presence of K₂CO₃, the brominated alcohol moiety of intermediate 184 first formed an epoxide, which then underwent ring-opening reaction with the aforementioned amine 183 to yield an amino alcohol; subsequent catalytic hydrogenation removed both benzyl groups to obtain afurotropine. Finally, afurotropine was salted with tartaric acid, yielding afurotropine tartrate 182 with a yield of 70%.

Storage Conditions

Store (2S)-HYDROXY(PHENYL)ACETIC ACID (2R)-N-BENZYL-1-(4-METHOXYPHENYL)PROPAN-2-AMINE (1:1) (SALT) in a tightly closed container at room temperature or 2–8°C, in a dry area. Protect from light. The salt is stable under these conditions for at least 36 months. No special inert atmosphere is required, although a desiccant pouch is recommended in humid environments.

Application Scenarios

1.Formoterol Fumarate API (GMP)

Serves as the official registered starting material for the formoterol side‑chain amine in many DMFs.

2.Arformoterol Tartrate API

Provides the necessary (2R)‑amine stereochemistry without chiral chromatography.

3.Generic Drug Development

Used in ANDA filings where a well‑characterized, compendial‑grade starting material is required.

4.Process Validation Batches

Stable, crystalline form facilitates accurate charging and reproducibility in pilot‑ and commercial‑scale batches.

5.Analytical Method Development

The salt and its diastereomeric counterpart are essential for developing and validating chiral purity methods.

Storage Conditions

Store (2S)-HYDROXY(PHENYL)ACETIC ACID (2R)-N-BENZYL-1-(4-METHOXYPHENYL)PROPAN-2-AMINE (1:1) (SALT) in a tightly closed container at room temperature or 2–8°C, in a dry area. Protect from light. The salt is stable under these conditions for at least 36 months. No special inert atmosphere is required, although a desiccant pouch is recommended in humid environments.

Contact Us

To secure your inventory of this essential formoterol side‑chain salt, or to discuss the specifications needed for your specific regulatory market, contact the Cosperpharm supply management team — we’ll prepare a detailed quotation and arrange for a retained sample to be sent directly to your analytical lab.