A process for preparation of (2s, 5r)- sulfuric acid mono-{[(4-aminopiperidin-4-yl) carbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1]-oct-6-yl} ester
By reacting formula (II) with formula (III) to form formula (IV), and then undergoing hydrogenolysis, sulfonation and trifluoroacetic acid treatment, efficient and stable (2S,5R)-sulfate mono-{[( 4-Aminopiperidine- 4-yl)carbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1]-oct-6-yl} ester compound solves the problems of low efficiency and unstable output of existing methods, Meet the needs of industrial production.
Patent Information
- Application Number
- CN201380074161.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2013-03-08
- Filing Date
- 2013-10-12
- Publication Date
- 2015-12-09
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Existing preparation of (2S,5R)-sulfate mono-{[(4-aminopiperidin-4-yl)carbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1]-octane -6-yl}ester compound method has low efficiency and unstable output, making it difficult to meet the needs of industrial production.
By reacting formula (II) with formula (III) to form formula (IV), followed by hydrogenolysis to form formula (V), then sulfonation to form formula (VI), and finally reaction with trifluoroacetic acid, it is converted into the target compound formula (I) . The process involves the use of suitable coupling agents, transition metal catalysts, solvents, and specific reaction conditions such as water, methanol, and sulfur trioxide-pyridine complexes.
Efficient and stable preparation of (2S,5R)-sulfate mono-{[(4-aminopiperidin-4-yl)carbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1 ]-oct-6-yl} ester compound, improves the yield and purity, and meets the requirements of industrial production.