Synthetic method of perdeuterated nitrogen heterocyclic compound
By using a hydrogen-deuterium exchange reaction with a palladium-on-carbon and sodium borohydride synergistic catalytic system, the problems of harsh reaction conditions and high cost in existing methods for synthesizing fully deuterated nitrogen heterocyclic compounds have been solved. This method achieves efficient deuteration and high yield under mild conditions and is applicable to the synthesis of a variety of nitrogen heterocyclic compounds.
Patent Information
- Application Number
- CN202610566624.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-04-27
- Publication Date
- 2026-06-30
AI Technical Summary
Existing methods for synthesizing fully deuterated nitrogen heterocyclic compounds suffer from drawbacks such as harsh reaction conditions (high temperature, hydrogen requirement), high cost of deuterium sources, narrow substrate applicability, and cumbersome synthesis steps. There is an urgent need to develop a synthesis method that has mild reaction conditions, is safe and reliable, uses inexpensive and readily available deuterium sources, has broad substrate applicability, and is easy to operate.
A synergistic catalytic system of palladium on carbon and sodium borohydride was adopted. Under nitrogen protection, nitrogen heterocyclic compounds, palladium on carbon catalyst, sodium borohydride co-catalyst and deuterium water were mixed to carry out hydrogen-deuterium exchange reaction to achieve the synthesis of fully deuterated nitrogen heterocyclic compounds, avoiding high temperature and the use of external hydrogen.
It achieves efficient deuteration under mild conditions, reduces production costs, expands the substrate applicability range, improves deuteration rate and yield, simplifies reaction operation, and is suitable for the full deuteration labeling of a variety of nitrogen heterocyclic compounds.