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  • Synthesis of 4-(2H-[1,2,4]-Triazol-5-ylsulfanyl)-1,2-dihydropyrazol-3-one via Ring-Switching Hydrazinolysis of 5-Ethoxymethylidenethiazolo [3,2-b][1,2,4]triazol-6-one

Aminoheterocycles as synthons for combinatorial Biginelli reactions

Mol. Diver. , 2011, 15 (1), 189-195

DOI: 10.1007/s11030-010-9253-6

Ryabukhin S.; Plaskon A.; Boron S.; Volochnyuk D.; Tolmachev A.

Chlorotrimethylsilane (TMSCl) has been utilized as an efficient promoter and water scavenger in the synthesis of diverse dihydropyrimidines via Biginelli type MCR-heterocyclization using aminoheterocycles. High yields and a simple workup of target compounds enable the facile generation of combinatorial libraries comprising more than 2 000 compounds of high structural and functional diversity. A representative set of 89 compounds is described.

Aminoheterocycles as synthons for combinatorial Biginelli reactions

Ryabukhin S.; Plaskon A.; Boron S.; Volochnyuk D.; Tolmachev A.
Mol. Diver. 2011, 15 (1), 189-195
DOI: 10.1007/s11030-010-9253-6

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