Invention:
This technology is an organocatalytic strategy that enables directly converting readily accessible aldehydes to their 1-deutero counterparts. The approach is distinct from the reported transition metal catalyzed ionic hydrogen-deuterium exchange (HDE) processes. The power of this new process has not only been demonstrated for aromatic aldehydes, but also for aliphatic substrates, which have been difficult for HDE, and for selective late-stage deuterium incorporation into complex structures with uniformly high deuteration level (>90%).
Background:
Among isotopes, deuterium has perhaps the broadest impact on almost every sub-discipline in the life, chemical, material, and nuclear sciences and beyond. The recent surge in applications of deuterated pharmaceutical agents has been witnessed by the FDA approval of the first deuterated drug, austedo (deutetrabenazine), in 2017, as well as the large number of emerging deuterated drug candidates. This has created an urgent demand for synthetic methods that enable the efficient generation of deuterated building blocks.
Applications:
- Synthesis of deuterated aldehydes
Advantages:
- Efficient
- Minimal steps
- Ability to produce a wide range of compounds
