Synthesis p. 147 - 149 (1995)
Update date:2022-08-31
Topics:
Ansari
Craig
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.
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(2000)