Tritium labelling and characterization of the antimalarial drug (+/-)-chloroquine by several methods.
To study its mechanism of antimalarial action, a tritium labelled analogue of (+/-)-chloroquine was required at high specific activity. Two synthetic methods were successfully employed. [3-3H] (+/-)-Chloroquine 2 was prepared by the catalytic tritium dehalogenation of an iodo precursor and [N-ethyl-3H] (+/-)-chloroquine 4 was synthesized by the alkylation of (+/-)-desethylchloroquine with [3H] ethyl iodide.
Egan
Judith A
JA
PerkinElmer Life Sciences, Inc., 549 Albany St., Boston, MA 02118, USA.
Laseter
Anne G
AG
Filer
Crist N
CN
D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry; D002738:Chloroquine / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013237:Stereoisomerism; D014316:Tritium / Q000737:chemistry*
D000962:Antimalarials; D014316:Tritium; D002738:Chloroquine