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Recent Advances in the Biginelli Dihydropyrimidine Synthesis. New Tricks from an Old Dog

Kappe, C. Oliver·2000·Accounts of Chemical Research

Abstract

In 1893, P. Biginelli reported the synthesis of functionalized 3, 4-dihydropyrimidin-2(1H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea, and ethyl acetoacetate. In the past decade, this long-neglected multicomponent reaction has experienced a remarkable revival, mainly due to the interesting pharmacological properties associated with this dihydropyrimidine scaffold. In this Account, we highlight recent developments in the Biginelli reaction in areas such as solid-phase synthesis, combinatorial chemistry, and natural product synthesis.

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Metadata

Authors
Kappe, C. O.
Venue
Accounts of Chemical Research
Published
2000-09-28
Volume
33
Issue
12
Pages
879-888
ISSN
  • 0001-4842 (ISSN-L)
  • 1520-4898
OpenAlex
W2127457669
Cited by
1,104
References
0
FWCI
13.65
Type
journal article
Language
en
Open access
closed

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CoChat. (2026). Citation check: Recent Advances in the Biginelli Dihydropyrimidine Synthesis. New Tricks from an Old Dog. https://app.cochat.ai/papers/10.1021/ar000048h
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Kappe, C. O. (2000). Recent Advances in the Biginelli Dihydropyrimidine Synthesis. New Tricks from an Old Dog. Accounts of Chemical Research. https://doi.org/10.1021/ar000048h

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