Pesti J A, Huhn G F, Yin J, Xing Y, Fortunak J M, Earl R A
Chemical and Physical Sciences Department, The DuPont Pharmaceuticals Company, Experimental Station, Wilmington, Delaware 19880-0500, USA.
J Org Chem. 2000 Nov 17;65(23):7718-22. doi: 10.1021/jo9804339.
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.
2-氟-4-甲基吡啶（3）通过氯化、水解和甲磺酰化高效官能化，转化为新型烷基化剂7。在精心设定的条件下，该甲磺酸盐用于蒽酮的双烷基化反应，以制备认知增强剂候选药物1。该过程的总收率高达37%，且适用于大规模合成。
