Efficient Pyridinylmethyl Functionalization: Synthesis of 10, 10-Bis [(2-fluoro-4-pyridinyl) methyl]-9 (10 H)-anthracenone (DMP 543), an Acetylcholine Release …

…, GF Huhn, J Yin, Y Xing, JM Fortunak…

文献索引：Pesti; Huhn; Yin; Xing; Fortunak; Earl Journal of Organic Chemistry, 2000 , vol. 65, # 23 p. 7718 - 7722

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被引用次数: 12

摘要

2-Fluoro-4-methylpyridine (3) is efficiently functionalized by chlorination, hydrolysis and methanesulfonylation 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.