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METHOD OF DIASTEREOSELECTIVE SYNTHESIS OF OPTICALLY ACTIVE CIS-NUCLEOSIDES, NUCLEOSIDE ANALOGS OR DERIVATIVES AND INTERMEDIATE COMPOUNDS FOR THIS METHOD
METHOD OF DIASTEREOSELECTIVE SYNTHESIS OF OPTICALLY ACTIVE CIS-NUCLEOSIDES, NUCLEOSIDE ANALOGS OR DERIVATIVES AND INTERMEDIATE COMPOUNDS FOR THIS METHOD
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机译:光学活性CIS-核苷,核苷类似物或衍生物和中间体化合物的非对映选择性合成方法
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FIELD: chemistry of nucleosides. SUBSTANCE: products: compounds of the formula (I): where R1 - hydrogen; R2 - pyrimidine base or its derivative; W - oxygen; X - group CH2,; Y - group CH2. Synthesis is carried out by glycosylation of pyrimidine base or its derivative with enantiomer compound of the formula (II): where R3 - lower alkoxycarbonyl; L - group OR where R - hydrogen or C1-C6-aliphatic acyl-group in the presence of Lewis acid of the formula (III): followed by reduction of glycosylated base or its derivative. Invention proposes also intermediate compounds of the formula (II) where W - oxygen; X = Y - CH2; R3- - lower alkoxycarbonyl; L - group OR where R - H or C1-C6--aliphatic acyl-group, and formula (VIII) where R2- - pyrimidine base or its derivative; R3- - lower alkoxycarbonyl used by this method. The synthesized compounds show high optical purity. EFFECT: improved method of synthesis, improved quality of compounds. 9 cl, 6 tbl
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机译:领域:核苷化学。物质:产品:式(I)的化合物:<图像文件=“ 00000001.GIF” he =“ 14” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 33” />其中R 1 < / Sub>-氢; R 2 Sub>-嘧啶碱基或其衍生物; W-氧气; X-CH 2 Sub>组; Y-组CH 2 Sub>。合成是通过嘧啶碱基或其衍生物与通式(II)的对映异构体化合物进行糖基化来完成的: “ />其中R 3 Sub>-低级烷氧羰基; L-基团OR,其中R-氢或在式(III)的路易斯酸存在下C 1 Sub> -C 6 Sub>-脂族酰基基团:<图像文件= “ 00000003.GIF” he =“ 18” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 16” />,然后还原糖基化碱基或其衍生物。本发明还提出了式(II)的中间化合物。<图像文件=“ 00000004.GIF” he =“ 10” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 30” />其中W-氧; X = Y-CH 2 Sub>; R 3 Sub>--低级烷氧羰基; L-组OR,其中R-H或C 1 Sub> -C 6 Sub>-脂肪族酰基,式(VIII)其中R 2 Sub>--嘧啶碱基或其衍生物; R 3 Sub>--该方法使用的低级烷氧羰基。合成的化合物显示出高的光学纯度。效果:改进了合成方法,提高了化合物的质量。 9厘升,6汤匙
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