ForMaMide, N-[5-(2R)-oxiranyl-2-(phenylMethoxy)phenyl]-

Formamide, N-[5-(2R)-oxiranyl-2-(phenylmethoxy)phenyl]- is a registered key starting material in the industrial synthesis of the long‑acting β₂‑adrenoceptor agonist formoterol fumarate and its single‑isomer analog arformoterol tartrate. The (2R)‑oxirane configuration of Formamide, N-[5-(2R)-oxiranyl-2-(phenylmethoxy)phenyl]- directly transfers to the (R)‑configured benzylic alcohol after epoxide opening with an enantiopure amine, locking in the correct absolute stereochemistry required for potent bronchodilation. Process chemists appreciate that Formamide, N-[5-(2R)-oxiranyl-2-(phenylmethoxy)phenyl]- is a stable crystalline solid, easily isolated and purified by crystallization, which dramatically reduces the reliance on preparative chiral chromatography. Cosperpharm supplies Formamide, N-[5-(2R)-oxiranyl-2-(phenylmethoxy)phenyl]- with strict chiral purity specifications, ensuring that the final API consistently meets the >99% diastereomeric excess standard demanded by regulatory authorities.

Product Parameters

Why Cosperpharm?

Cosperpharm manufactures Formamide, N-[5-(2R)-oxiranyl-2-(phenylmethoxy)phenyl]- using a route that minimizes epoxide ring‑opening by‑products and formamide hydrolysis, two degradation pathways that compromise yield and chiral purity. Our process controls the final crystallization so that the product is delivered as a free‑flowing, single‑polymorph powder, eliminating concerns about polymorph variability during formulation. Each batch is released against a comprehensive analytical panel including chiral HPLC (≥99.5% e.e.), achiral HPLC (≥99.0%), and specific optical rotation, giving your production team a starting material with unambiguous stereochemical identity. We ship under refrigerated, argon‑blanketed conditions, and we can provide full documentation — including residual solvents, heavy metals, and genotoxic impurity assessment — formatted for direct inclusion in your DMF amendment or ASMF.

Product Advantages

1. Absolute Chiral Transfer – The (2R)‑epoxide opens with inversion at the oxirane carbon, directly setting the (R)‑benzylic alcohol configuration essential for formoterol and arformoterol activity.

2. Stable, Crystalline Chiral Intermediate – Unlike many epoxide intermediates that are oils or require freezer storage, this compound is a crystalline solid stable at 2–8°C.

3. Orthogonal Protecting Group Strategy – The formamide (latent aniline) and benzyl ether (latent phenol) can be sequentially deprotected under mild hydrogenolysis or acidic conditions.

4. High Purity = Fewer Purifications – ≥99.0% achiral purity and ≥99.5% e.e. reduce the need for downstream recrystallization of the final API.

5. Commercial‑Scale Availability – Cosperpharm can supply from 100‑g qualification samples to multi‑kilogram production batches under the same validated process.

Storage Conditions

Store Formamide, N-[5-(2R)-oxiranyl-2-(phenylmethoxy)phenyl]- at 2–8°C in a tightly sealed, light‑resistant container under an inert gas such as argon or nitrogen. Protect from moisture and any sources of heat or acidic vapors. Do not store near reactive nucleophiles. If the container has been opened, replace the inert gas blanket and apply Parafilm. Under these conditions, shelf life is confirmed as 24 months.

Contact Us

When your next formoterol or arformoterol campaign requires a chiral epoxide building block backed by complete regulatory documentation, contact Cosperpharm’s API intermediates team — we can arrange a technical call with our process chemists to review your proposed route and provide a delivery schedule aligned with your ANDA submission timeline.