Abstract:The synthesis of a series of 2- and 8-substituted 4-amino-7-chloroquinolines is presented. The chloro in the 7-position can be effectively substituted using amino alcohols to yield novel analogues of the antimalarial (hydroxy)chloroquine. Both short chain (2-aminoethanol) and long chain (5-[N-ethyl-N-(2-hydroxyethyl)amino]-2-aminopentane) coupling partners can be used. While ketone and nitro functionalities were found to be incompatible with the coupling conditions, electron-donating amino and dimethylamino su… Show more
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