Solid Phase Synthesis of 3,4,5-Trisubstituted-1,2,4-Triazoles Derivatives from the Resin-Bound Acylhydrazines

• 作者: Chao Mai Rongjian Xie Xingang Liu Zhanxiang Liu
• 来源期刊: 有机化学国际期刊(英文)
• 学科: 化学
• 关键词: Resin-Bound Acylhydrazine Solid-Phase Synthesis 1 2 4-Triazoles
• 年，卷（期）: 2013,（1）
• 页码范围: 35-40
• 页数: 6页
• 分类号: O6

摘要

An extension of our methodology on solid-phase synthesis of 3,4,5-trisubstituted-1,2,4-triazoles under mild conditions has been developed. Firstly, the resin-bound acylhydrazine is reacted with orthoesters to provide resin-bound 1,3,4-oxadiazoles. Secondly, condensation of 1,3,4-oxadiazoles resin with the corresponding arylamines hydrochloride to form the the resin-bound triazoles. 3,4,5-Trisubstituted-1,2,4-triazoles derivatives were obtained from resin-bound acylhydrazines in several steps providing 78% - 87% overall yields and excellent purity. The advantages of this method include straightforward operation and high yield and purity of the products.