Making Anti-Tuberculosis Drug Bedaquiline Affordable by Tackling Low-Yielding Key Steps

Bedaquiline is a new and innovative antibiotic against Mycobacterium, but the synthesis of the molecule has made the drug difficult to manufacture. Herein, a systematic approach to significantly increase the efficiency of the synthesis is presented that will make the drug available. The study centers on the key alkylation step that builds up the crowded quaternary adjacent to a tertiary center.