4.8 Review

Synthetic Entries to and Biological Activity of Pyrrolopyrimidines

Journal

CHEMICAL REVIEWS
Volume 116, Issue 1, Pages 80-139

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.chemrev.5b00483

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Funding

  1. Research Foundation Flanders (FWO Vlaanderen)
  2. UGent Special Research Fund (UGent BOF)
  3. Agency for Innovation by Science and Technology [IWT/100014/SBO]

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This review summarizes recent literature (2000-2015) on the synthesis and pharmaceutical properties of pyrrolopyrimidines. These modified pyrimidine bases, fused to a pyrrole ring, and their corresponding nucleosides display a broad applicability in medicinal chemistry. This overview is divided into three main sections, according to the respective isomers: pyrrolo[2,3-d]pyrimidines, pyrrolo[3,2-d]pyrimidines, and pyrrolo[3,4-d]pyrimidines. Each section contains a description of common retro-synthetic strategies, with particular attention for newly reported synthetic entries to the scaffold. Next, the synthetic strategies and the ways in which the scaffolds can be further modified are exemplified according to the biological properties of the obtained products.

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