Establishment of systematic chemical synthetic method of element substitution type nucleic acid oligomer which becomes the next generation nucleic acid drug candidate

2023 Fiscal Year Final Research Report

• Project/Area Number: 19H00930
• Research Category: Grant-in-Aid for Scientific Research (A)
• Allocation Type: Single-year Grants
• Section: 一般
• Review Section: Medium-sized Section 38:Agricultural chemistry and related fields
• Research Institution: Tokyo University of Agriculture and Technology
• Principal Investigator: Chiba Kazuhiro 東京農工大学, (連合)農学研究科(研究院), 学長 (20227325)
• Co-Investigator(Kenkyū-buntansha): 岡田 洋平 東京農工大学, (連合)農学研究科(研究院), 准教授 (80749268)
• Project Period (FY): 2019-04-01 – 2023-03-31
• Keywords: 核酸医薬 / 電解合成 / 化学合成 / 中分子

Outline of Final Research Achievements

Many azanucleosides have a basic structure in which oxygen atoms are replaced by nitrogen atoms in the natural nucleic acid structure, and exhibit superior functions and activities to those of conventional nucleic acid drug candidates. In this study, we developed a systematic synthesis method for various azanucleoside derivatives, which are difficult to achieve by conventional methods, by advancing the chemical synthesis of intermediate molecules based on the organic electrolytic reaction method and the reverse micellar liquid phase reaction. We have established an innovative manufacturing method to efficiently obtain oligomers composed of azanucleoside units in a very short process.

Free Research Field

生物有機化学

Academic Significance and Societal Importance of the Research Achievements

The efficient and innovative chemical synthesis method that can supply large quantities of high-purity products of substances that are expected to be used as raw materials for pharmaceuticals is expected to dramatically expand the knowledge of their activities.