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- W2034858980 abstract "Abstract 9‐Amino‐8‐fluoro‐2, 4‐methano‐1,2,3,4‐tetrahydroacridine citrate (SM‐10888), a novel cholinesterase inhibitor, was labeled with carbon‐14 at C9 of the tetrahydroacridine ring for use in metabolic studies. Carbonation of 2,6‐difluorophenyllithium ( 3 ) with [ 14 C]carbon dioxide gave the acid ( 4 ). Chlorination of 4 followed by treatment of the resulting acid chloride with ammonia afforded the amide ( 5 ). Dehydration of 5 with thionyl chloride and subsequent displacement reaction with ammonia gave the aminobenzonitrile ( 7 ). Condensation of 7 with the ketone ( 8 ) in the presence of anhydrous zinc chloride yielded the aminoacridine ( 9 ), which was treated with citric acid to afford [9‐ 14 C]SM‐10888 ( 1 ). The overall yield of 1 was 37% from 2 , and the specific activity was 1.35 GBq/mmol." @default.
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- W2034858980 date "1992-07-01" @default.
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- W2034858980 title "14C-labeling of a tetrahydroacridine, a novel CNS-selective cholinesterase inhibitor" @default.
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- W2034858980 doi "https://doi.org/10.1002/jlcr.2580310707" @default.
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