Novel, low-cost, and environmentally friendly pathway for synthesizing tigecycline

Abstract

The development of tigecycline, effective against tetracycline-resistant bacteria, began with the synthesis of its precursor, 9-amino minocycline, derived from minocycline hydrochloride through nitration. Water served as the primary solvent, ensuring cost-effective processing. In the final step, conversion to tigecycline required only tert-butylglycinoyl chloride hydrochloride as a reactant. This method shows great potential for the sustainable production of tigecycline, making it more accessible for large-scale use as an antibiotic. Throughout the synthesis, various techniques such as IR, ¹H NMR, ¹³C NMR, and mass spectrometry were used to characterize each product at different stages.