二萜内脂化合物的制备方法
By employing an oxidant and a palladium catalyst in the synthesis of triptolide alcohol, a hydroxyl or alkoxy group is directly introduced at the C14 position, solving the problem of high cost in existing technologies and realizing a new method for the efficient preparation of triptolide intermediates with a yield of over 77%.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SHANGHAI LINKCHEM TECHNOLOGY CO LTD
- Filing Date
- 2023-09-28
- Publication Date
- 2026-07-17
AI Technical Summary
In the existing technology, when synthesizing intermediate compounds 3a or 3b of triptolide alcohol or triptolide ketone, there is a lack of a direct method to introduce the hydroxyl or alkoxy group at the C14 position, resulting in high production costs and difficulty in derivatization.
A method is used to introduce carbonyl, hydroxyl, or alkoxy groups at specific reaction sites using an oxidant. Compound 1 is reacted with the oxidant to generate compound 2, which is then converted to compound 3a or 3b in the presence of a palladium catalyst and solvent under an oxygen atmosphere. The specific steps include using chromium trioxide as the oxidant, palladium catalyst, and specific solvent, and controlling the reaction conditions to achieve efficient conversion.
This method enables the efficient introduction of hydroxyl or alkoxy groups at the C14 position, opening up new routes for the preparation of triptolide or its derivatives, improving production efficiency, and providing a new path for C14-position derivatization, with yields exceeding 77%.
Smart Images
Figure CN117384233B_ABST