THE PREPARATION OF D-RING-CONTRACTED ANALOGS OF QINGHAOSU (ARTEMISININ) FROM QINGHAO (ARTEMISINIC) ACID AND THEIR IN-VITRO ACTIVITY AGAINST PLASMODIUM-FALCIPARUM

被引：19

作者：

HAYNES, RK ^{[1
]}

VONWILLER, SC ^{[1
]}

WANG, HJ ^{[1
]}

机构：

[1] UNIV SYDNEY,DEPT ORGAN CHEM,SYDNEY,NSW 2006,AUSTRALIA

来源：

TETRAHEDRON LETTERS | 1995年 / 36卷 / 26期

基金：

澳大利亚研究理事会;

关键词：

D O I：

10.1016/0040-4039(95)00806-N

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Qinghao (Artemisinic) acid was converted into dihydroqinghao aldehyde and then submitted to copper(II)-catalysed oxidative deformylation. The resulting ketone was reduced to the diastereomeric alcohols which were submitted to photooxygenation, and then cleavage-oxygenation-cyclisation, catalysed by Cu(II)(OSO2CF3)(2), to give the title compounds. In vitro testing results for antimalarial activity indicated a remarkable dependence on the stereochemistry of the 9-methyl-substituent.

引用

页码：4641 / 4642

页数：2

共 11 条

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