(R)-5,7-difluorochroman-4-ol

(R)-5,7‑Difluorochroman‑4‑ol is a critical chiral intermediate in the industrial synthesis of tegoprazan, a novel P‑CAB indicated for GERD and erosive oesophagitis. The chiral chromanol scaffold of (R)-5,7‑Difluorochroman‑4‑ol provides the essential three‑dimensional framework for tegoprazan‘s activity as a H⁺/K⁺ ATPase inhibitor. The R‑configuration at C4 is critical for biological activity, making enantiopurity a paramount quality attribute of (R)-5,7‑Difluorochroman‑4‑ol. The fluorine substituents at the 5‑ and 7‑positions enhance metabolic stability and lipophilicity, contributing to the favourable pharmacokinetic profile of tegoprazan. In quality control contexts, (R)-5,7‑Difluorochroman‑4‑ol is designated as Tegoprazan Impurity 8, serving as an important reference standard for analytical method development and impurity profiling. The compound is also of interest in medicinal chemistry programs targeting neuroprotective agents and enzyme inhibitors, demonstrating the versatility of (R)-5,7‑Difluorochroman‑4‑ol beyond tegoprazan synthesis.

 

Product Parameters

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Parameter	Specification
Product Name	(R)-5,7-Difluorochroman-4-ol
CAS Number	1270294057
Molecular Formula	C₉H₈F₂O₂
Molecular Weight	186.16 g/mol
Boiling point	228.4±40 °C
Density	1.402±0.06 g/cm3
pKa	13.09±0.20
Appearance	White solid
Storage Condition	2–8 °C

Application

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R-5,7-Difluorochroman-4-ol is a heterocyclic organic compound that can be used as an intermediate for the synthesis of tegoprazan. Tegoprazan is a hydrogen/potassium ion exchange aChemicalbooktpase (H+/K+ ATPase) inhibitor and competitive potassium-competitive acid blocker (P-CAB), mainly used for the treatment of gastroesophageal reflux disease and erosive esophagitis.

 

Synthetic Route

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R-5,7-difluorochroman-4-ol is obtained by asymmetric reduction reaction using 5,7-difluorochroman-4-one as the substrate in the presence of a ketoreductase, a coenzyme and a coenzyme recycling system.

 

Why Cosperpharm?

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When your tegoprazan manufacturing campaign demands enantiopure chiral intermediates, Cosperpharm delivers (R)-5,7‑Difluorochroman‑4‑ol with the analytical rigor and documentation depth that pharmaceutical customers require.

 

Enantiopurity is non‑negotiable. The R‑configuration at C4 is critical for tegoprazan‘s biological activity. Any racemisation will compromise your final API. Our release protocol includes chiral HPLC verification and specific rotation analysis to ensure enantiomeric excess meets your specifications.

 

Fluorination for improved properties. The 5,7‑difluoro substitution pattern enhances metabolic stability and bioavailability. We provide detailed analytical data confirming the correct substitution pattern and fluorination.

 

Dual‑use intermediate and impurity standard. Supplied as both a synthetic intermediate and as Tegoprazan Impurity 8 for analytical method development.

 

Documentation for regulatory submission. Every shipment includes a comprehensive COA. DMF‑ready documentation and custom quality agreements are available.

 

Contact Us

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Need (R)-5,7‑Difluorochroman‑4‑ol for your tegoprazan program? Cosperpharm is your trusted source for fluorinated chiral intermediates. Contact us today—we‘re ready to support your project from research through commercial production.