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Alkyne-modified deoxyadenosine phosphoramidite monomer and preparation method thereof

A technology of deoxyadenosine phosphoramidite and deoxyadenosine, which is applied in the field of medicine and can solve problems such as high cost, restrictions on practical application, and complex synthesis methods

Active Publication Date: 2022-06-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the synthesis method of deoxynucleosides containing unnatural bases is complex, with many steps and high cost, which restricts its practical application in DNA labeling and functionalization

Method used

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  • Alkyne-modified deoxyadenosine phosphoramidite monomer and preparation method thereof
  • Alkyne-modified deoxyadenosine phosphoramidite monomer and preparation method thereof
  • Alkyne-modified deoxyadenosine phosphoramidite monomer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Pour pH=7.0, 5ml of 0.1mol / L phosphate buffer solution into a 10ml round-bottomed flask. Add to round bottom flask

[0034] Get 100mg of compound 1 in a single-neck round bottom flask (10ml), dissolve with 5ml of purified water. Prepare 5mol / L NaOH

Embodiment 2

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PUM

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Abstract

The invention belongs to the technical field of medicine, and discloses a synthesis method and an application of an alkynyl-modified deoxyadenosine phosphoramidite monomer compound. In the present invention, the N6 position of deoxyadenosine is carboxylated, and then modified by alkynyl group to obtain an intermediate, and the alkynyl-modified deoxyadenosine phosphoramidite is obtained through two-step reaction of the protection of the 5' terminal hydroxyl group and the 2' terminal phosphoramidite reaction. monomer compound. Through the solid-phase synthesis of DNA, it is introduced into the oligonucleotide at a specific site to obtain an oligonucleotide modified with an alkyne group at a specific site. The invention applies the alkynyl-modified deoxyadenosine phosphoramidite monomer compound to the alkynyl modification of the oligonucleotide, and the method is simple and the yield is considerable. It provides new ideas and valuable intermediates for the subsequent functionalization of DNA, and has broad application prospects.

Description

A kind of alkynyl modified deoxyadenosine phosphoramidite monomer and preparation method thereof technical field The invention belongs to the technical field of medicine, relate to the deoxyadenosine phosphoramidite monomer compound of alkynyl modification, especially It relates to a deoxyadenosine phosphoramidite monomer compound modified by an alkynyl group at the adenine base site, and the present invention also relates to the alkynyl group-containing Preparation method and application of modified adenosine phosphoramidite monomer compound. Background technique In recent years, with the development of nucleic acid chemical synthesis technology, a series of chemical modifications have been reported in academia and industry. oligonucleotide derivatives. Chemical modifications of oligonucleotides include sugar ring, base site modification, phosphodiester backbone Modifications, or substitution of chemical structures with specific functions for natural nucleosides, e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/207C07H21/04C07H1/00
CPCC07H19/207C07H21/04C07H1/00Y02P20/55
Inventor 刘明哲王诗宇
Owner SHENYANG PHARMA UNIVERSITY