3056-13-1Relevant academic research and scientific papers
4 - Thiodeoxythymidine derivative and anti-hepatitis B virus pharmaceutical application thereof
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Paragraph 0019, (2021/10/05)
4 - Thio-deoxythymidine derivatives and anti-hepatitis B virus pharmaceutical applications thereof are disclosed. The invention provides 4 - thiodeoxythymidine derivative or a pharmaceutically acceptable salt thereof, and the structure is shown in structural formula I or structural formula II. An in-vitro cytotoxicity test and an in-vitro anti HBV virus pharmacodynamic test proves 4 - thiodeoxythymidine derivative or a pharmaceutically acceptable salt thereof has anti HBV activity, has an anti-hepatitis B drug development prospect and provides a potential choice for treating viral hepatitis.
Method for preparing high-purity telbivudine compound
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, (2017/01/02)
The invention belongs to the technical field of medicine and provides a method for preparing a high-purity telbivudine compound. The method includes the steps that an LTD-4 compound serves as the raw material and reacts with thymine subjected to silicification protection, and an intermediate, namely an LTD-5 compound, can be obtained; then, through deprotection reaction, the telbivudine compound is obtained after post-processing, wherein MeONa serves as an alkaline reagent of the deprotection reaction, and strong-acidity resin serves as a dealkalization reagent. The method simplifies the production process, the yield of each step is high, and a target product high in purity and yield is obtained. Please see the structural formula in the description.
Synthesis of beta-L-2'-deoxy nucleosides
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Page/Page column 19-30; 40; 41, (2010/02/11)
An improved process for the preparation of 2′-modified nucleosides and 2′-deoxy-nucleosides, such as, β-L-2′-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2′-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2′-anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2′-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2′-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2′-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.
Methods of manufacture of 2'-deoxy-beta-L-nucleosides
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Page/Page column 22-23, (2008/06/13)
The present invention relates to the synthesis of 2′-deoxy-β-L-thymidine, 2′-deoxy-β-L-uridine and 2′-deoxy-β-L-cytidine, and their derivatives, such as the 3′-O-acyl or 3′,5′-O-diacyl prodrugs, including the 3′-O-L-aminoacyl and 3′,5′-O-L-diaminoacyl prodrugs, and particularly the 3′-O-L-valinyl and 3′,5′-O-L-divalinyl prodrugs.
OLIGODEOXYRIBONUCLEOTIDES
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, (2008/06/13)
An oligodeoxynucleotide including an oligonucleotide comprising 5'-phosphates of a nucleoside, formed by combining 2-deoxy-L-erythro-pentose with a nucleic acid base in the form of a β-anomer, linked with each other through 3'→5' phosphodiester linkages;
