Synthesis of S-(+)-rivastigmine hydrogentartrate / 南方医科大学学报
Journal of Southern Medical University
;
(12): 177-180, 2007.
Article
in Chinese
| WPRIM
| ID: wpr-298212
ABSTRACT
<p><b>OBJECTIVE</b>To optimize the synthetic procedure of S-(+)-rivastigmine hydrogentartrate which was known as an agent for the treatment of Alzheimer disease.</p><p><b>METHODS</b>S-(+)-rivastigmine hydrogentartrate was synthesized by using 1-(3-hydroxyphenyl)ethanone as the starting material via oximation, reduction and N-methylation to produce the key intermediate 3-1-dimethylaminoethylphenol, which finally reacted with N-ethyl-N-methylcarbamoyl chloride. The enantiomers were resolved with di-(+)-p-toluoyl-D-tartaric acid, and the title compound was prepared by mixing S-rivastigmine base with L-(+)-tartrate.</p><p><b>RESULTS</b>The total yield of S-(+)-rivastigmine hydrogentartrate was 4.17%.</p><p><b>CONCLUSION</b>The materials in this procedure are all commercially available. The reaction conditions are mild and total yield is high.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Stereoisomerism
/
Molecular Structure
/
Chemistry
/
Cholinesterase Inhibitors
/
Phenylcarbamates
/
Rivastigmine
/
Models, Chemical
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2007
Type:
Article
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