215674-15-0Relevant articles and documents
Efficient pyridinylmethyl functionalization: Synthesis of 10,10-bis[(2-fluoro-4-pyridinyl)methyl]-9(10H)-anthracenone (DMP 543), an acetylcholine release enhancing agent
Pesti,Huhn,Yin,Xing,Fortunak,Earl
, p. 7718 - 7722 (2007/10/03)
2-Fluoro-4-methylpyridine (3) is efficiently functionalized by chlorination, hydrolysis and methane-sulfonylation into the novel alkylating agent 7. This mesylate is used for the bisalkylation of anthrone under carefully defined conditions to prepare the cognition enhancer drug candidate 1. This process proceeds in up to 37% overall yield and is adaptable for large scale synthesis.
2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action
Earl, Richard A.,Zaczek, Robert,Teleha, Christopher A.,Fisher, Barbara N.,Maciag, Carla M.,Marynowski, Maria E.,Logue, Andrew R.,Tam, S. William,Tinker, William J.,Huang, Shiew-Mei,Chorvat, Robert J.
, p. 4615 - 4622 (2007/10/03)
In an effort to improve the pharmacokinetic and pharmacodynamic properties of the cognition-enhancer linopirdine (DuP 996), a number of core structure analogues were prepared in which the 4-pyridyl pendant group was systematically replaced with 2-fluoro-4