Work

Solid-Phase Synthesis of Guanine Derivatives with Four Diversity Elements via AgNO3-Mediated Guanidine Formation

Year: 2025

Type: article

Abstract: High Resolution Image Download MS PowerPoint Slide We constructed a guanine derivative library with four diversities through efficient solid-phase synthesis. In this reaction, thiourea was transformed into guanidine through a guanylation reaction using AgNO 3, and the guanine core was synthesized by cyclization using a base. After oxidation using m CPBA, several nucleophiles were substituted to construct 36 derivative libraries through solid-phase synthesis. The reaction involved 7 steps in total, showing a good yield of over 57–82%, but it also showed a difference in cyclization reaction selectivity between solid-phase synthesis and solvent-phase synthesis. We will use the synthesized chemical library to find hit compounds for various diseases.

Source: ACS Omega

DOI: 10.1021/acsomega.5c08443

Authors: Jimin Moon, Jimin Lee, Hyojin Lee, Geonho Yoon, Taeho Lee

Institutions: Kyungpook National University, Daegu-Gyeongbuk Medical Innovation Foundation

Language: English

Topic: Chemical Synthesis and Analysis

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: gold

Estimated APC paid: $1,935

Funders: Kyungpook National University, National Research Foundation of Korea