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

Rongjian Xie, Xingang Liu, Chao Mai, Zhanxiang Liu
2013 International Journal of Organic Chemistry  
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 1,3,4oxadiazoles. Secondly, condensation of 1,3,4-oxadiazoles resin with the corresponding arylamines hydrochloride to form the resin-bound triazoles. 3,4,5-Trisubstituted-1,2,4-triazoles derivatives were obtained from resin-bound acylhydrazines in several steps
more » ... veral 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.
doi:10.4236/ijoc.2013.31a004 fatcat:2oivi3h7ufcr7nutqv7coln6ry