[Preparation of albendazole sulfoxide--- an active metabolite]
1College of Pharmacy, Zhejiang University, Hangzhou 310031, China.
Abstract:
OBJECTIVE: To investigate the facile method for preparation of albendazole sulfoxide, an active metabolite in vivo. METHODS: The reaction condition was investigated according to evaluations to the results of the experiment through temperature, solvent, oxidation agent, reaction time and impurity. RESULTS: The target compound was obtained by oxidation of albendazole with the presence of sodium metaperiodate in glacial acetic acid under low temperature and was free from contamination by impurity albendazole sulfone. Pure product (content >98%) and high yield (>90%percnt;) have been achieved due to reaction selection. CONCLUSION: Oxidation condition is essential to the preparation of albendazole sulfoxide.
Related Concept Videos
Preparation and Reactions of Sulfides
Drug Biotransformation: Overview
Drug Metabolism: Phase II Reactions
Phase I Reactions: Oxidation of Aliphatic and Aromatic Carbon-Containing Systems
Oxidation reactions are fundamental in aromatic carbon-containing systems. An example is the hydroxylation of phenobarbital, a process that transforms it into...
Phase II Reactions: Glucuronidation
Phase II Reactions: Sulfation and Conjugation with α-Amino Acids


