- Synthesis process of (2R')-2'-deoxyl-2'-fluoro-2'-methyluridine
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The invention discloses a synthesis process of (2R')-2'-deoxyl-2'-fluoro-2'-methyluridine, relates to the technical field of synthesis of medicines, and solves the technical problems of high cost andlow product yield of the existing process. According to the synthesis process, sodium borohydride or potassium borohydride is used for reducing ribose lactone, so that an expensive reductive reagent which is sodium dihydro-bis-(2-methoxyethoxy)aluminate or lithium tri-tert-butoxyaluminum hydride is not used, and the cost is greatly reduced; N,O-bis(trimethylsilyl)acetamide is used as a silicon etherification reagent, so that the yield of glycosylation reaction is increased; the product yield can reach 85-90% and is far higher than that in route III by 58%; the product yield is obviously increased; hydroxyl at the 5' site is protected, so that side reaction in ring-closing reaction can be avoided; meanwhile, a common polar solvent which is dimethylformamide is used; the product yield undercatalysis of sodium hydrogen carbonate can reach 87-92%. The synthesis process is easy to operate; the process condition is more easily controlled; the cost is reduced; the synthesis process is applicable to large-batch production.
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Paragraph 0022; 0051; 0060
(2018/09/13)
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- Facile synthesis of 2-C-methyl-D-arabino-γ-1,4-lactones and mechanism study
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In our previous research on the synthesis of 3,5-di-O-benzoyl-2-C-methyl-D-arabino-γ-lactone 4a, the reaction mechanism of DMSO-mediated configuration inversion of C2 hydroxyl group in the lactone was ambiguous. As a follow-up to this research, we used s
- Lv, Bingqing,Guo, Shuang,Zhu, Fuqiang,Hu, Tianwen,Guo, Qi,Lin, Haixia,Xie, Yuanchao,Shen, Jingshan
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supporting information
p. 1473 - 1475
(2018/03/13)
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- Preparation method and intermediate body of (2S, 3R, 4R)-3,5-bis-sustituted-2-deoxy-2-hydroxy-2-methyl-D-ribose-gamma-lactone
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The invention relates to a preparation method and an intermediate body of (2S, 3R, 4R)-3,5-bis-sustituted-2-deoxy-2-hydroxy-2-methyl-D-ribose-gamma-lactone. The intermediate body has the structure as shown in formula II. A compound in the formula II serves as the intermediate body for preparing (2S, 3R, 4R)-3,5-bis-sustituted-2-deoxy-2-hydroxy-2-methyl-D-ribose-gamma-lactone, stereoselectivity is good, the yield is high, reaction conditions are mild, raw materials 2-C-methyl-D-ribonic acid-1,4 lactone for preparing the intermediate body are wide in source, preparation is easy, and cost is low.
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Paragraph 0077; 0078; 0079; 0080
(2016/10/09)
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- A neighboring group participation strategy: Facile synthesis of 3,5-di-O-benzoyl-2-C-methyl-d-arabino-γ-lactone
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A simple and efficient approach for the synthesis of 3,5-di-O-benzoyl-2-C-methyl-d-arabino-γ-lactone through a neighboring group participation mechanism is reported. This compound could be a useful precursor for the synthesis of nucleoside antiviral agents.
- Xie, Yuanchao,Zhang, Jian,Tian, Guanghui,Xu, Mingshuo,Hu, Tianwen,Jiang, Xiangrui,Shen, Jingshan
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supporting information
p. 4345 - 4348
(2015/06/22)
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- Process for the preparation of ribofuranose derivatives
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The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of formula (I): useful in the synthesis of nucleotides.
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- PROCESS FOR THE PREPARATION OF RIBOFURANOSE DERIVATIVES
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The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of Formula (I) useful in the synthesis of nucleotides.
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Page 11-12;20-21
(2008/06/13)
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