一种制备新药砌块(6-甲酰基吡啶-3-基)氨基甲酸叔丁酯的方法
The preparation of (6-formylpyridin-3-yl) tert-butyl carbamate via a three-step synthetic route solves the synthetic difficulties in the existing technology, and realizes the preparation of new drug building blocks with high purity and high yield, which is suitable for industrial application.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SHANGHAI RUIPU PHARM TECH CO LTD
- Filing Date
- 2023-05-18
- Publication Date
- 2026-07-17
AI Technical Summary
There is a lack of effective synthetic methods in the current technology to prepare (6-formylpyridin-3-yl)carbamate tert-butyl ester, which is an important member of the new drug building block family.
A three-step synthetic route was adopted, which included reacting methyl 5-aminopyridine-2-carboxylate with an acylation reagent to generate methyl 5-(tert-butoxycarbonyl)amino)pyridine-2-carboxylate, followed by reaction with a reducing reagent to generate tert-butyl (6-(hydroxymethyl)pyridine-3-yl)carboxylate, and then reaction with an oxidizing reagent to generate tert-butyl (6-formylpyridine-3-yl)carboxylate. The reactions were carried out using readily available starting materials and relatively mild conditions.
It achieves the preparation of products with high purity and high yield, is simple to operate, suitable for industrial production, does not use hazardous reagents, and has a convenient purification process.
Smart Images
Figure CN116554092B_ABST