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Beilstein J. Org. Chem. 2025, 21, 217–225, doi:10.3762/bjoc.21.13
Graphical Abstract
Figure 1: Heteroannulated pyrimidones in drug discovery: blockbuster drugs that are based on the privileged p...
Scheme 1: Strategies towards targeted adducts: A) Niementowski quinazoline synthesis utilizing anthranilic ac...
Scheme 2: Access to the key building blocks 2–4 by employing three different nonisocyanide-based MCRs. Divers...
Scheme 3: Synthesis of N-substituted thienopyrimidones 5a–e by a Gewald three-component reaction employing 2-...
Scheme 4: Synthesis of N-substituted quinolinopyrimidones 6a–e from 2-aminoindoles 3a–e and formamide as C1 s...
Scheme 5: Synthesis of N-substituted indolopyrimidones 7a–e from 2-aminoindoles 4a–e and formamide as C1 sour...
Figure 2: Representative fluorescence spectrum of compounds 5b (λex = 330 nm) and 6e (λex = 430 nm) at 0.2 M ...
Figure 3: Molecular geometry observed within the crystal structure of compound 7b (CCDC 2376493).
Beilstein J. Org. Chem. 2019, 15, 513–520, doi:10.3762/bjoc.15.45
Scheme 1: MCR approach to indole-based macrocycles; a more effective strategy is proposed in this work, based...
Scheme 2: Reaction of unprotected diamines 3 with cyclic anhydrides 4 at rt affording α,ω-amino acids 5 in qu...
Scheme 3: Ugi macrocyclization in a one-pot fashion and synthesis of diverse indole-based macrocycles. The ci...
Figure 1: (A) Modeling of the macrocycle 2h (cyan sticks) and 2n (magenta sticks) into the MDM2 receptor (PDB...
Figure 2: (A) Overlay of 1 H,15N-HSQC spectra of the reference MDM2 (red) and the titration steps with the 2i...