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