A kind of preparation method of 3'-oxygen-methoxyethyl nucleoside

A technology for methoxyethyl nucleoside and methylcytosine, which is applied in the field of nucleoside compound synthesis, can solve the problem of difficulty in large-scale production, no method suitable for industrialized preparation of 3'-oxy-methoxyethyl nucleoside, and low yield And other issues
CN108424432BActive Publication Date: 2021-04-23SHANGHAI ZHAOWEI TECH DEV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI ZHAOWEI TECH DEV
Publication Date
2021-04-23

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Abstract

The invention discloses a preparation method of 3'-oxy-methoxyethyl nucleoside. The method comprises the steps of: (1) condensing a compound with a structure shown in formula B and a silylated protected base to obtain a compound with a structure shown in formula C; the base is selected from thymine, 5-methyl Cytosine, adenine or 2,6-diaminopurine; and (2) the 3'-oxygen-methoxyethyl nucleoside whose structure is shown in formula A is obtained through alkaline hydrolysis reaction by the compound shown in formula C ;
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Description

technical field

[0001] The invention relates to the field of nucleoside compound synthesis, in particular to a preparation method of 3'-oxygen-methoxyethyl nucleoside. Background technique

[0002] In recent years, with the development of genome-based drugs, antisense oligonucleotide drugs have been rapidly developed. The reason is that compared with traditional drugs, antisense oligonucleotide drugs have the following advantages, such as stronger specificity and greater information content. Because it acts on the upstream of the transmission of genetic information, the required dose is lower and the side effects are also less.

[0003] 3'-Oxy-methoxyethyl nucleoside is an analogue of the second generation antisense oligonucleoside, which is the basic raw material for nucleoside synthesis. 3'-O-methoxyethyl nucleosides can be used in scientific research, especially functional genomics research, in addition to being used as a drug development tool. However, the existing lit...

Claims

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