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Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Additive-Free Construction of Tetrahydropyrimidine Skeleton by using 1,3,5-Triazinane as Four-Atom Synthon
Lanlan Rong1, Jingwen Ma1, Chenru Lai1
1Key Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Diseases of Ministry of Education and School of Pharmacy, Gannan Medical University, Ganzhou 341000, P. R. China.
Abstract:
Herein, an unprecedented [4 + 2] cycloaddition of enaminone with 1,3,5-triazinane has been developed. The representative semihydrogenated aromatic heterocycle 1,2,3,4-tetrahydropyrimidines have been synthesized with a broad substrate scope, demonstrating potential antitumor activity. This approach has been smoothly conducted under additive-free and environmentally friendly conditions that are compatible with various functional groups. Furthermore, the condition optimization process reveals that the tetrahydropyrimidine product is regulated via the reaction temperature.
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