An Efficient Solvent‐Free, Catalyst‐Free Amination on Modified Nucleosides and One‐Pot Three‐Component Synthesis of 1,2,3‐Triazole‐Based Hybrid Nucleosides

Abstract

An efficient catalyst‐free, solvent‐free amination reaction has been developed for the synthesis of various bio‐inspired 6‐substituted amino purine nucleoside analogues in good yields. In this sustainable approach, unprotected 6‐substituted aminopurine nucleoside analogues were synthesized via amination reactions of unprotected 6‐Cl purine nucleosides with various amine derivatives. Notably, this method offers a simple, eco‐friendly, unifying protocol for the synthesis of various bioinspired molecules with highly functional group tolerance. Additionally, to demonstrate its synthetic applicability, a one‐pot, three‐component reaction protocol has been shown for the synthesis of novel 1,2,3‐triazole‐attached hybrid nucleoside containing various drug core moieties via click chemistry.