Suzhou Ribo Life Science Company, Ltd.

Suzhou Ribo Life Sciene Co., Ltd.

Shenzhen Ying Biopharmaceutical Co., Ltd

Zhen Xi

Jinyu Huang

Zicai Liang

Dan Wang

Junbin Zhang

Zhenghua Wang

Liqiang Cao

Disclosed are a cyclic dinucleotide prodrug molecule, a preparation method therefor and an application thereof relating to the field of pharmaceuticals. The cyclic dinucleotide prodrug molecule has a structure shown in formula I, II, or III, can freely cross cell membranes and release cyclic dinucleotide, and has high cell activity.

Cyclic dinucleotide prodrug molecule, preparation method therefor and application thereof

Nucleotide and/or oligonucleotide represented by formula (1) and the liquid phase synthesis process thereof. The present invention provides a liquid phase synthesis process for preparing a nucleotide and/or an oligonucleotide, comprising a process for combining the nucleotide and/or oligonucleotide protective groups, in which, under the condition that the 2'-hydroxyl group is protected by a group with a sterically hindered silane structure, the 3&#x2032; phosphate group(s) of the nucleotide and/or oligonucleotide is/are directly protected by (a)&#x3b2;-cyanoethyl group(s), and after the &#x3b2;-cyanoethyl group(s) is/are removed, the resulting product can directly participate in the next cycle of synthesis, wherein the synthesis reaction is carried out in a reaction flask or reaction kettle, without being limited by a solid carrier or synthesizer, so that the large scale preparation of oligonucleotides can be achieved. 

Nucleotide and/or oligonucleotide and preparation process thereof

A method for preparing oligonucleotide comprising reacting the compound of Formula (1) with the compound of Formula (2) in a liquid reaction medium under the condition of condensation reaction to obtain the compound of formula (3) is provided. 1-(2-mesitylenesulfonyl)-3-nitro-1H-1,2,4-triazole (MSNT) is applied as condensing agent. Oligonucleotides synthesized in the liquid reaction medium could be obtained on a large scale. 

Method for preparing oligonucleotide

Growing community of inventors

Tianjin, China

Zhen Xi