簡易合成2-氯-3-取代-5-甲氧基砒啶結構衍生物並應用於ABT-594的半合成研究

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Title:	簡易合成2-氯-3-取代-5-甲氧基砒啶結構衍生物並應用於ABT-594的半合成研究 A Versatile Approach to 2-Chloro-3-Substituted-5-Methoxypyridine Skeleton and Application to the Formal Synthesis of ABT-594
Authors:	郭展志
Contributors:	林敬涵嘉南藥理科技大學：藥物科技研究所
Keywords:	半合成 2-氯-3-取代-5-甲氧基砒啶 [3+3] 環合反應親核取代反應 [3+3] cycloaddition nucleophilic addition 2-ch
Date:	2009
Issue Date:	2010-06-09 09:34:25 (UTC+8)
Abstract:	關於2-氯-砒啶酯類的結構在nAChR接收器上有一系列的文獻報導，例如ABT-594、ABT-98593R與WJ-314313等都含有2-氯-砒啶的結構，它們被認為具有各種多樣的生物活性，因此而受到釵h注意。在結構活性的研究中，ABT-594含氮的四員環部份和2-氯-吡啶環都被證實有強力的止熱鎮痛活性，目前已有許多關於這些化合物合成的相關文獻，而我們成功發展出有效的合成2-氯-3-取代-5-甲氧基砒啶結構的方法，我們認為這方法可以有效的促進應用於ABT-594衍生物的合成研究上。 A considerable amount of literature has been published concerning the pyridylethers as nicotinic cholinergic receptor ligands(nAChR). For example, ABT-594，ABT-98593R，WJ-314313 have received much attention owing to variety of their biological activities. Numerous syntheses of these classes of compounds have been reported. Structure-activity studies of analogs related to ABT-594 suggest that the N-unsubstituted azetidine moiety and the 2-chloro substituent on the pyridine ring are important contributors to potent analgesic activity. We have successfully developed an efficient approach to 2-chloro-3-substituted-5-methoxypyridines，this methodology had proved to be applicable for the synthesis of ABT-594
Relation:	校內校外均不公開，學年度：97，90 頁
Appears in Collections:	[Dept. of Pharmacy] Dissertations and Theses

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