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 bioinspired 6-substituted aminopurine nucleoside analogs in good yields. In this sustainable approach, unprotected 6-substituted aminopurine nucleoside analogs are synthesized via amination reactions of unprotected 6-Cl purine nucleosides with various amine derivatives. Notably, the 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 nucleosides containing various drug core moieties via click chemistry.