Abstract

A method for forced oxidative mechanochemical degradation of active pharmaceutical ingredients (APIs) using clopidogrel hydrogensulfate as a model compound is presented. Considerable and selective formation of degradants occurs already after very short reaction times of less than 15 minutes and the nature of the products is strongly dependent on the used oxidant.

Highlights

  • A method for forced oxidative mechanochemical degradation of active pharmaceutical ingredients (APIs) using clopidogrel hydrogensulfate as a model compound is presented

  • In particular we became interested in producing oxidative degradants avoiding commonly used solutions like H2O2, which often result in complex degradation profiles or even irrelevant products due to harsh conditions, undesired reaction pathways and strong solvent effects

  • HPLC analysis of reaction mixtures obtained after using KMnO4 showed the presence of one main degradant with a retention time of approximately 10 min (Fig. S3, Electronic supplementary information (ESI)†)

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Summary

Introduction

A method for forced oxidative mechanochemical degradation of active pharmaceutical ingredients (APIs) using clopidogrel hydrogensulfate as a model compound is presented.

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