Synthesis and Characterization of Bromoclenbuterol

Ravi Kumar Kannasani,Srinivasa Reddy Battula

doi:10.4172/2161-0444.1000397

Abstract

Clenbuterol is a sympathomimetic amine used for breathing disorders as a decongestant and bronchodilator. During the process development of clenbuterol, the process related impurity bromoclenbuterol was identified as a critical impurity along with the final API. The present work describes the synthesis and characterization of this bromoclenbuterol.

Highlights

Clenbuterol, it is most commonly available as the hydrochloride salt, clenbuterol hydrochloride
Among the six process related impurities, the bromoclenbuterol impurity was identified as a critical impurity and it was formed in the synthesis of clenbuterol hydrochloride active pharmaceutical ingredient (API) at the time of chlorination of 4-amino acetophenone (Table 1)
It is the one of by product in Stage-I reaction. It will form in the synthesis of 4-Amino-This impurity can be controlled by using crystallization

Summary

Introduction

Clenbuterol, it is most commonly available as the hydrochloride salt, clenbuterol hydrochloride. Among the six process related impurities, the bromoclenbuterol impurity was identified as a critical impurity and it was formed in the synthesis of clenbuterol hydrochloride API at the time of chlorination of 4-amino acetophenone (Table 1). Reaction mixture was poured in to chilled water, obtained precipitate was filtered, dried and recrystallized in methanol to give 5 gm (yield-82%) of 1RS-1-(4-amino -3-bromo-5-chloro phenyl) -2-[(1,1-dimethyl ethyl)amino ethanol (or) Bromo clenbuterol (10) as off-white solid.

Objectives

Results

Conclusion