Arylsubstituted the oil - and anthraquinones having anti-hiv activity

 

The invention relates to new chemical substances, specifically to arylsubstituted the oil - and anthraquinones of formula I:where (a)-g) R=H; h) R=OMe; a) X=7-hydroxy-2-methyl-1,4 - naphthoquinone-5-yl; b) X= 7-hydroxy-2-methyl-6-etoxycarbonyl-1,4-naphthoquinone-5-yl; C) X=3-hydroxy-9,10-anthraquinone-1-yl; g) X= 8-hydroxy-3-trimethyl-siloxy-2-etoxycarbonyl-and 1,1, 4,4-Tetra-hydro-9,10-anthraquinone-1-yl; d) X=8-hydroxy-3-oxo-1,2,3,4-tetrahydro-9,10-anthraquinone-1-yl; (e) X=3-hydroxy-2-taxicab-Nile-4,4-dihydro-9,10-anthraquinone-1-yl; g) X= 3,8-dihydroxy-2-etoxycarbonyl-4,4-dihydro-9,10-anthraquinone-1-yl; C) X= 3-hydroxy-2-etoxycarbonyl-4,4-dihydro-9,10-anthraquinone-1-yl, possessing anti-HIV activity. The compounds are non-toxic, does not have side effects. 3 table.

Description text in facsimile form (see drawings) PM

Claims

Arylsubstituted the oil - and anthraquinones, the General formulawhere (a) - g) R= H; h) R= OMe; a) X= 7-hydroxy-2-methyl-1,4-naphthoquinone-5-yl; b) X= 7-hydroxy-2-methyl-6-etoxycarbonyl-1,4-naphthoquinone-5-yl; C) X= 3-hydroxy-9,10-anthraquinone-1-yl; g) X= 8-hydroxy-3-trimethyl-siloxy-2-etoxycarbonyl-and 1,1, 4,4-Tetra-hydro-9,10-anthraquinone-1-yl; d) X= 8-hydroxy-hydroxy-2-etoxycarbonyl-4,4-dihydro-9,10-anthraquinone-1-yl; C) X= 3-hydroxy-2-etoxycarbonyl-4,4-dihydro-9,10-anthraquinone-1-yl, possessing anti-HIV activity.

 

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The invention relates to a new process for the preparation of substituted anthraquinones represented by the General formula (I)

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in which R denotes H or a linear or branched alkyl with from 1 to 5 carbon atoms, R1means HE or alloctype containing from 1 to 5 carbon atoms, and R2means N, by the Diels-alder reaction between 1,4-naftochinona General formula (II)

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in which R1specified above, and X represents H or chlorine, with acyclic diene of the General formula (III) CH2= CR-CH=CH-OR3(III) in which R is specified above, and R3means a group of the formula-Si(R4)3where R4means a linear or branched C1-C5alkyl group, in the presence of catalytic amounts of hydroquinone with obtaining substituted tetrahydrogestrinone General formula IV

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where R, R1, R3above, followed by reaction of the oxidative removal of the protective group with Jones reagent to obtain the substituted anthraquinone General formula (I)

The invention relates to a new process for the preparation of substituted anthraquinones represented by the General formula (I)

< / BR>
in which R denotes H or a linear or branched alkyl with from 1 to 5 carbon atoms, R1means HE or alloctype containing from 1 to 5 carbon atoms, and R2means N, by the Diels-alder reaction between 1,4-naftochinona General formula (II)

< / BR>
in which R1specified above, and X represents H or chlorine, with acyclic diene of the General formula (III) CH2= CR-CH=CH-OR3(III) in which R is specified above, and R3means a group of the formula-Si(R4)3where R4means a linear or branched C1-C5alkyl group, in the presence of catalytic amounts of hydroquinone with obtaining substituted tetrahydrogestrinone General formula IV

< / BR>
where R, R1, R3above, followed by reaction of the oxidative removal of the protective group with Jones reagent to obtain the substituted anthraquinone General formula (I)

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