| 摘要 |
The invention is used for the preparation of biologically active compounds containing cyclic peroxyacetallactone or lactol functional groups, in particular qinghaosu (Artemisinin). By the method compounds are produced containing peroxyacetal, peroxyacetallactol or peroxyacetalether functional group, oxidattion occurring in the presence of one or more oxidant metallic catalysts of a compound containing hydroperoxyalkene carboxylic acid, hydroxyperoxyalkenealdehyde, hydroperoxyalkeneketone group or their dialkylacetals and a hydroperoxyalkenealcoholic functional group. The method is performed by the following scheme: where n has the value of 1, 2 or 3, m is 0, 1 or 2, p is 0, 1, 2 or 3; R5 means the groups -COON, -CROH, -C(O)R or where R is H, alkyl, aryl or arylalkyl; R1 means separately alkyl, arylalkyl or every R1 together with the group -O-C-O-, to which it is attached forms cyclic acetal; X means CR2R3, O, S, SO, SO2 where R2 and R3 are selected independently among H, optionally substituted alkyl or aryl, and when n is more than 1, X is selected independently and can be with a straight or branching chain and together with substituent Y can form a ring; Y is substituent selected among H, optionally substituted alkyl or aryl; Y can be positioned at the same C atom where the hydroxyperoxy group is and any C atom can be double-substituted by Y in the substitution of H atom(s) in the (CH2)m group by Y; R6 or R7 have the meanings listed above for R, H, OH, OR or, together with the carbon atom to which they are attached, form a ketogroup.
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