Synthesis of pyrrolo[3,2-d]pyrimidine-2,4(3H)-diones by domino C–N coupling/hydroamination reactions

• Ruben Manuel Figueira de Abreu,
• Robin Tiedemann,
• Peter Ehlers and
• Peter Langer

Beilstein J. Org. Chem. 2025, 21, 1010–1017, doi:10.3762/bjoc.21.82

• to develop novel pharmaceuticals with improved biological properties. For instance, pemetrexed (F) is administered during palliative chemotherapy for advanced lung cancers [12]. Immucillin H (G) is currently in late clinical phases for the treatment of haematologic diseases, such as acute T-cell

• activities. Development of drugs based on pyrrolopyrimidines: A: Cadeguomycin. B: Tubercidin. C: Toyocamycin. D: Batzelladine A. E: Sangivamycin. F: Pemetrexed. G: Immucillin H. H: TAK-285 (tyrosine kinase inhibitor). UV–vis absorption (left) and emission (right, λex = 300 nm) spectra of compounds 4a, 4j, 4k

Structural diversity in the host–guest complexes of the antifolate pemetrexed with native cyclodextrins: gas phase, solution and solid state studies

• Magdalena Ceborska,
• Magdalena Zimnicka,
• Aneta Aniela Kowalska,
• Kajetan Dąbrowa and
• Barbara Repeć

Beilstein J. Org. Chem. 2017, 13, 2252–2263, doi:10.3762/bjoc.13.222

• /bjoc.13.222 Abstract The complexation of the antifolate pemetrexed (PTX) with native cyclodextrins was studied. This process, along with the findings gathered for the structurally related folic acid was treated as a model for exploiting host–guest interactions of this class of guest molecules in the

• ; pemetrexed; supramolecular chemistry; Introduction Herein, supramolecular host–guest complexes of the potent folic acid inhibitor pemetrexed (PTX, Figure 1a) with native cyclodextrins (α-, β- and γ-CDs, Figure 1b) in the gas phase (MS), in solution (NMR, UV–vis) and in the solid state (Raman, FTIR–ATR) were

• complexes is a highly attractive way to overcome these unwanted features [8]. One of such chemotherapeutic drugs is pemetrexed (PTX), developed initially in 2004 for the treatment of non-small lung cancer [9]. This type of cancer is the most commonly appearing cancer in the world [10] and its treatment