7488-24-6Relevant articles and documents
Entecavir intermediate and its preparation method
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, (2017/12/28)
The invention discloses an entecavir intermediate and a preparation method thereof. A provided preparation method for an entecavir intermediate compound 8 comprises the following steps: performing hydroxyl protection group removal reaction on a compound 9 in a solvent under an acidic condition, so as to obtain the compound 8. A provided preparation method for an entecavir intermediate compound 9 comprises the following steps: performing hydroxyl protection group adding reaction on a compound 10 in an aprotic organic solvent under an alkali condition, so as to obtain the compound 9. The preparation methods are cheap and easily available in raw materials, mild in reaction conditions, relatively high in product yield, good in atom economy, friendly to environment, and suitable for industrialized production.
Entecavir intermediate and its preparation method
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Paragraph 0380; 0385-0386; 0388; 0395, (2017/12/28)
The invention discloses an entecavir intermediate and a preparation method thereof. A provided preparation method for an entecavir intermediate compound 10 comprises the following steps: performing reducing reaction on an ester compound 11 in an organic solvent under the effect of a reducing agent, so as to obtain the compound 10. A provided preparation method for an entecavir intermediate compound 11 comprises the following steps: reacting a compound 12 with a hydroxyl protection reagent in an organic solvent in the presence of an acid to add a hydroxyl protection group, so as to obtain the compound 11. The preparation methods are cheap and easily available in raw materials, mild in reaction conditions, relatively high in product yield, good in atom economy, friendly to environment, and suitable for industrialized production.
A kind of preparation method of the midbody of entecavir, and intermediate
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Paragraph 0392; 0393; 0399, (2017/08/02)
The invention discloses Entecavir intermediates and a preparation method thereof. The preparation method of an Entecavir intermediate represented by a formula VIII shown in descriptions comprises the following step of enabling compounds IX and VIII' to be subjected to ring cleavage reaction in the presence of alkali in a non-aprotic organic solvent. The invention further discloses an Entecavir intermediate compound represented by a formula X or IX shown in descriptions. The preparation method disclosed by the invention has the advantages that raw materials are cheap and are easily obtained, the reaction conditions are mild, side reactions are few, the yield is high, the pollution to the environment is little, and the intermediates are easily purified and separated, so that the preparation method is applicable to industrial production.