Selective incorporation of deuterium in place of hydrogen (deuteration) has the unique effect of retaining the biochemical potency and selectivity of physiologically active compounds while, in select instances, modifying metabolic fate to substantially alter their overall therapeutic profile. In favorable cases, this modification has the potential to have a positive effect on safety, efficacy and/or tolerability. However, due to almost identical physical and chemical properties (polarity, boiling point, melting point, and others), the deuterium-containing molecule and non-deuterium-containing one CAN NOT be separated by current isolation technologies such as distillation, recrystallization, sublimation, SiO2-column separation, etc. So far, no technology has been reported for the separation of a deuterium-containing compound from the corresponding hydrogen-containing one except for D2O/H2O. Therefore, the only approach to date to make deuterium-containing drugs is to start with high purity (&gt; 99%) deuterium-containing intermediates which today are mainly simple molecules, such as NMR solvents (CD3OH, CD3CD2OH, and CD3COCD3). This restriction means that the use of current organic synthesis methods for the production of deuterium-containing drugs is severely limited to those compounds that can be produced from these simple starting materials. CombiPhos utilizes a totally different approach for the preparation of deuterium-containing drugs from those methods currently in use by many pharmaceutical companies. The Company developed a novel catalysis method to selectively replace hydrogen atoms with deuterium atoms. This unique process is NOT based on available high-purity deuterium-containing starting materials. More importantly the Company’s unique technology is able to selectively substitute a deuterium atom(s) for one or more hydrogen atoms in a targeted drug, while still achieving a deuterium compound purity as high as 99%.

Preparation of deuterated drugs through novel catalysis:  Synthesis, purification, and preclinical data

253rd National Meeting (2017)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.