Process for the production of optically active pyrrolidine compounds
By using a base and a chiral catalyst in a bilayer solvent system of hydrophobic solvents and water to carry out the addition reaction of malonic acid derivatives with nitrostyrene derivatives, the problems of slow reaction rate and safety were solved, and the industrial production of optically active pyrrolidine compounds with high yield and enantioselectivity was achieved.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- TANABE PHARMA CORP
- Filing Date
- 2018-01-30
- Publication Date
- 2026-07-07
AI Technical Summary
In the existing technology, the addition reaction between malonic acid derivatives and nitrostyrene derivatives has problems such as slow reaction rate, low yield and poor enantioselectivity. At the same time, the crystalline form of nitrostyrene derivatives poses an explosion hazard, which leads to unsafe industrial production.
In a bilayer solvent system of hydrophobic solvent and water, an addition reaction of malonic acid derivatives with nitrostyrene derivatives is carried out using a base and a chiral catalyst. This avoids the crystalline form of the nitrostyrene derivatives, improves the reaction yield and enantioselectivity, and allows for multiple consecutive steps to ensure safety.
This method achieves high-yield and enantioselective addition reactions, avoids the handling of explosive intermediates, and improves the safety and economy of industrial production.
Smart Images
Figure CN116854624B_ABST