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[Synthesis of 14C-azelastine hydrochloride]
Arzneimittel-Forschung
|January 1, 1983
Summary
The synthesis of 14C-azelastine hydrochloride, a potential pharmaceutical compound, was achieved using 14C-phthalic anhydride as the starting material. This study details the chemical pathway for creating this isotopically labeled drug candidate.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Radiochemistry
Context:
- Azelastine hydrochloride is an established pharmaceutical agent.
- The development of radiolabeled compounds is crucial for drug metabolism and pharmacokinetic studies.
- Phthalazinone derivatives have shown diverse pharmacological activities.
Purpose:
- To describe the synthetic route for 14C-azelastine hydrochloride.
- To establish a method for producing a radiolabeled version of azelastine for research purposes.
- To utilize 14C-phthalic anhydride as a key precursor in the synthesis.
Summary:
- The synthesis of 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride, specifically labeled with Carbon-14 (14C-azelastine hydrochloride, Asta A 5610), was successfully accomplished.
- The synthetic process commenced with 14C-phthalic anhydride as the foundational starting material.
- This provides a reliable method for generating isotopically labeled azelastine.
Impact:
- Enables detailed studies on the absorption, distribution, metabolism, and excretion (ADME) of azelastine.
- Facilitates pharmacokinetic and pharmacodynamic investigations of azelastine.
- Supports the development and regulatory approval of azelastine-based therapies through comprehensive preclinical research.