A convenient, short synthesis of desethylchloroquine [7-chloro-4-(4'-ethylamino-1'-methylbutylamino)quinoline]
A short, efficient 2-step synthesis of desethylchloroquine is achieved by generating an internal amide ion from the secondary nitrogen in chloroquine, followed by in situ reaction with 2,2,2-trichloroethyl chloroformate giving rapid elimination of ethylene. The carbamate thus produced easily undergoes deprotection to the target compound at room temperature.
Ansari,Craig
p. 147 - 149
(2007/10/02)
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