Explorations into Eszopiclone.pptVIP

Explorations into Eszopiclone 顾岩 0440803 李梦婕 0440723 魏雪莹 0440123 单纯 0440105 Outlines Introduction SAR and Synthesis Mechanism and drug effect Clinical application and Side effects Prospects of Eszopiclone and Comparison between similar drugs Introduction SAR Synthesis The separation of enantiomers Introduction of Eszopiclone Eszopiclone belongs to the group of medicines called central nervous system (CNS) depressants (medicines that make you drowsy or less alert). This medicine is used to treat insomnia (trouble in sleeping, helping you get to sleep faster and sleep through the night. The Enationmers Zopiclone was produced and developed by Rhdne-poulenc company in France. It hit the French market in 1987 with its commercial name “Imovane”. Eszopiclone The S-enantiomer of zopiclone Eszopiclone was approved by the US Food and Drug Administration on December 15, 2004, for the treatment of insomnia in patients aged _18 years. Its commercial name is “Lunesta”. Before the development of zopiclone, there are many sedative-hypnotic drugs which are used for the treatment of insomnia. These drugs include antihistamines, sedating anti-depressants, neuroleptics, benzodiazepines, non-benzodiazepine receptor agonists and melatonin. Although the structure of zopiclone is quite different with that of benzodiazepines, it can bind with benzodiazepine receptors and has similar pharmacoactivity with benzodiazepines. Since its side effects are much fewer than benzodiazepines, it is categorized to the third generation of sedatives . pyrrolo-piperazine ring 5-choloro pyridine ring carbonyl group piperazine formyl group Synthesis of Zopiclone Derivatives Studies show that the affinity of (S)-zopiclone to the receptor is 1000 times larger than (R)-zopiclone, and (R)-zopiclone has nearly no sedative and hypnotic effects. As a result, scientists began to study the ways that they can get the pure (S)-enationmer of zopiclone. Separation of Enationmers The most wi