- Uracil nucleoside derivative and method for preparing deoxyuridine drug by using same (by machine translation)
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The invention discloses (I) deoxy - D D-furan ribose 5 - styryl 1 - [2 - (1 - benzoate) derivative represented by the formula] and a preparation method, of the derivative, wherein the structure of the general formula (I) is shown. And the preparation method (I) of, deoxy - D D-furan ribose 5 - styryl 1 - [2 - (1 - benzoate) derivatives as above reaction raw materials can be used as a glycosyl donor to activate] under the conditions of the catalytic amount of the Lewis acid trifluoromethanesulfonate and N - iodosuccinimide, and, reaction efficient, yield 98%. reaching, is avoided in the conventional reaction system using an equivalent or excess of a Lewis acid, benzoyldiimide as a glycosyl donor. (by machine translation)
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Paragraph 0077-0080
(2020/05/14)
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- A Doxifluridine synthetic method
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The invention relates to a synthesis method of doxifluridine: will be 5 - Fluorouracil, hexamethyldisilazane and ammonium sulfate refluxing reaction, the resulting double-silicon ether 5 - Fluorouracil with 5 - deoxy - triacetyl ribose in added to the methylene chloride, into the tin tetrachloride, obtained reaction liquid; the reaction liquid is poured into the clean water for hydrolysis, then layered, organic layer by the alkaline concentration recovery dichloromethane, to obtain core intermediate 2 ', 3' - O - di-ethyl - 5 - fluoro uracil nucleoside; intermediate adding ammonia in methanol solution to carry out saponification reaction, after the reaction, concentrating and recovering methanol, to get the crude product, refined crystal to obtain Doxifluridine. The method of the invention using a cheap and easily obtained 5 - fluoro uracil and 5 - deoxy - triacetyl ribose as raw materials, through the silicon ether, condensation, hydrolysis and saponification four-step reaction synthesizes Doxifluridine, greatly simplifying the production process, shortens the reaction time, the reaction is more complete, high-purity product.
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Paragraph 0017; 0018; 0019; 0020
(2018/06/16)
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- Rapid continuous synthesis of 5′-deoxyribonucleosides in flow via Br?nsted acid catalyzed glycosylation
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A general, green, and efficient Br?nsted acid-catalyzed glycosylation serves as a key step in the one-flow, multistep syntheses of several important 5′-deoxyribonucleoside pharmaceuticals.
- Shen, Bo,Jamison, Timothy F.
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supporting information; experimental part
p. 3348 - 3351
(2012/08/08)
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- Design, synthesis and anti-tumoractivity of novel amidine derivatives of doxifluridine
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A series of novel amidine derivatives of doxifluridine were synthesized using acid amide as the starting material, and their anti-tumor activity was evaluated in A549 cells. Compounds 10 and 11 demonstrated were more potent than 5-Fu, which was used as a positive control. Compound 10, which were found to be the most potent one with IC50 of 3.2 μmol/L, was 16 times more potent than 5-Fu with IC50 of 52 μM to the A549 cells. A new route was designed to synthesize 5′-deoxy-5-fluorocytidine. All compounds were characterized by 1H NMR, MS and X-ray spectras in detail.
- Feng, Ji Lu,Sun, Hai Ling,Geng, Dong Ping,Li, Ke
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scheme or table
p. 163 - 166
(2010/11/18)
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