氯喹的代谢产物：关于去乙基氯喹和N-乙酰去乙基氯喹的一些观察结果。

Metabolites of chloroquine: some observations on desethylchloroquine and N-acetyldesethylchloroquine.

作者信息

Ansari A M, Craig J C

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 94143-0446.

出版信息

J Pharm Sci. 1994 Jul;83(7):1040-2. doi: 10.1002/jps.2600830722.

DOI:10.1002/jps.2600830722

PMID:7965661

Abstract

The major metabolite of chloroquine, (+)-desethylchloroquine, produced by stereoselective N-dealkylation of the drug, was obtained in 81.5% enantiomeric purity by resolution of racemic desethylchloroquine using an atropisomeric resolving agent and was shown by circular dichroism to have the absolute (S)-configuration. The minor metabolite N-acetyldesethylchloroquine was prepared in both the racemic and the (S)-(+)-form.

摘要

氯喹的主要代谢产物，即通过该药物的立体选择性N-脱烷基化产生的(+)-去乙基氯喹，使用一种阻转异构拆分剂拆分外消旋去乙基氯喹，以81.5%的对映体纯度获得，并通过圆二色性表明其绝对构型为(S)-型。次要代谢产物N-乙酰去乙基氯喹以外消旋体和(S)-(+)-型两种形式制备。