7488-24-6Relevant articles and documents
A kind of preparation method of the midbody of entecavir, and intermediate
-
Paragraph 0386; 0388; 0392; 0399; 0400, (2017/08/02)
The invention discloses Entecavir intermediates and a preparation method thereof. The preparation method of an Entecavir intermediate represented by a formula IV or IV' shown in descriptions comprises the following step of enabling a compound V to be subjected to amino protecting group and hydroxyl protecting group removal reaction in the presence of protonic acid in a solvent. The preparation method disclosed by the invention has the advantages that raw materials are cheap and are easily obtained, 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.
Entecavir intermediate and its preparation method
-
Paragraph 0373; 0381-0383; 0385; 0387; 0395-0396; 0398, (2017/10/28)
The invention discloses an entecavir intermediate and a preparation method thereof. A provided preparation method for an entecavir intermediate compound 3 comprises the following steps: performing reducing reaction on a compound 4 in a solvent, so as to obtain the compound 3. A provided preparation method for an entecavir intermediate compound 4 comprises the following steps: performing transacetalation reaction on a compound 5 and a compound 18 in an organic solvent under an acid condition, so as to obtain the compound 4. 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
-
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.