Abstract:
PROBLEM TO BE SOLVED: To provide compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, methods for preparing such compounds, and intermediates obtained during such methods.SOLUTION: This invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof [L1 is -O- or NRa-; A is -Ar2-L2-Ar3; Ar2 is 5- or 6-membered monocyclic heteroaryl; Ar3 is heteroaryl; L2 is a bond; and Ra is hydrogen or alkyl].
Abstract translation:要解决的问题:提供作为氮杂金刚烷衍生物的化合物,特别是醚或胺取代的氮杂金刚烷衍生物及其盐和前药,包含这些化合物的组合物,使用这些化合物和组合物的方法,制备这些化合物的方法和获得的中间体 在此方法中。本发明涉及式(I)化合物或其药学上可接受的盐[L1是-O-或NRa-; A是-Ar2-L2-Ar3; Ar2是5-或6-元单环杂芳基; Ar 3是杂芳基; L2是一个债券; 和Ra是氢或烷基]。
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing a condensed bicyclic heterocycle-substituted aza bicyclic compound represented by the following formula (8).SOLUTION: A specified condensed bicyclo heterocycle-substituted aza bicyclic compound is treated with specified halo-substituted benzene iodide in the presence of CuI, 1,10-phenanthroline and Cs2CO3 to form a phenyl ether derivative. The same is treated with hexamethyditin or the like in the presence of a palladium catalyst to form a tin compound. The same is further treated with Ar2-halo (Ar2 is a condensed 9-membered bicyclic heteroaryl ring; and the halo is bromine, chlorine or iodine) to obtain a compound in the formula (8).