我们报告了允许访问两个氧杂环应变中间体,4,5-苯并呋喃和 3,4-氧杂环己炔的合成方法。这些中间体的原位捕获通过形成一个或多个新的 CC 或 C-杂原子键提供了一系列杂环支架。实验确定的区域选择性与使用失真/相互作用模型所做的预测一致,并且还发现与在相应含氮中间体的捕获实验中看到的选择性相比更大。这些研究证明了氧杂环芳烃和炔烃在合成功能化杂环方面的多功能性,同时进一步扩大了变形/相互作用模型的范围。而且,
我们报告了允许访问两个氧杂环应变中间体,4,5-苯并呋喃和 3,4-氧杂环己炔的合成方法。这些中间体的原位捕获通过形成一个或多个新的 CC 或 C-杂原子键提供了一系列杂环支架。实验确定的区域选择性与使用失真/相互作用模型所做的预测一致,并且还发现与在相应含氮中间体的捕获实验中看到的选择性相比更大。这些研究证明了氧杂环芳烃和炔烃在合成功能化杂环方面的多功能性,同时进一步扩大了变形/相互作用模型的范围。而且,
The present invention relates to a compound of the formula [1′]
1
wherein R
2
is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R
5
is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R
5
may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.
The present invention relates to a compound of the formula [1' ]
wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, -O-,-S- and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1' ] as an active ingredient The compound [1' ] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1' ] as a nociceptin antagonist or analgesic.