Aminoheterocycles as synthons for combinatorial Biginelli reactions
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Updated: Jun 13, 2026

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Sergey V Ryabukhin1, Andrey S Plaskon, Sergey Yu Boron
1Enamine Ltd, 23 A. Matrosova St., Kyiv, 01103, Ukraine. Ryabukhin@mail.enamine.net
Abstract:
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.
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