A second generation focused library of 30 tetrahydropyrimidinone amides was prepared. The design was based on the structure of an Hsp70 modulator. This small library demonstrates the utility of tandem multi-component reactions in structure-activity relationship studies of biological lead molecules. The tandem Biginelli-Ugi multi-component reaction facilitated the effective variation of four different substituents and allowed the synthesis of the library members in a sequence of only two one-pot reactions.
Biginelli reactions - Ugi reactions - cascades - Hsp70 - pyrimidinones