Traditional approaches to developing complex pharmaceuticals, such as antibiotics, are based on semi-synthetic production. These approaches have yielded many valuable products, but have limited the range of potential chemical diversity that can be developed from a core molecule. This, in turn, limits the range of potential biological activities that can be carried out. Historically, only minor structural changes could be made to core chemical structures produced via microbial fermentation. Nearly all semi-synthetic efforts have been directed at a small number of core intermediates, and this lack of chemical diversity has led to limitations in anti-infective diversity.

The process allows Tetraphase to unlock the chemical diversity of the tetracycline class by leveraging this novel, modular, flexible, synthetic platform and this has already yielded an unprecedented series of structurally diverse analogs.

"The synthesis...is not just a synthetic tour de force; it enormously expands the armamentarium of the Tetracycline medicinal chemist."

– A New Route to Designer Antibiotics by Chaitan Khosla of Stanford University and Yi Tang of UCLA (C&E News, Chemistry review), Science, Vol 308, April 15 2005