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Updated: May 10, 2026

Preparation of N-(2-alkoxyvinyl)sulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Parallel synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones on solid-phase
Miao Hu1, Wei Huang, Marc A Giulianotti
1Institute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou 310058, P.R. China.
Abstract:
A parallel solid-phase synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones from MBHA resin is described. The reduction of resin-bound nitrosamino acids provides hydrazines efficiently without affecting the amide bond. The trityl protected hydrazine is then reduced with borane, and cyclized with 1,1-carbonyldiimidazole. The desired products are cleaved from their solid support and obtained in good yield and purity. This methodology is of value for the rapid parallel preparation of these potentially bioactive molecules.
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