4.4 Article

Biginelli reaction: an overview

Journal

TETRAHEDRON LETTERS
Volume 57, Issue 47, Pages 5135-5149

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2016.09.047

Keywords

Biginelli reaction; Dihydropyrimidinones; Multicomponent reaction; Aldehyde; Urea; Active methylene compound

Funding

  1. Science and Engineering Research Board (SERB), New Delhi
  2. Science and Engineering Research Board, New Delhi [B/FT/CS-152/2014]
  3. Council of Scientific and Industrial Research (CSIR), New Delhi

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Biginelli reaction involves acid-catalyzed one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) using easily-accessible starting materials, namely, aldehyde, active methylene compound and (thio)urea. DHPMs have stimulated resurgence of interest in the past two decades due to their wide ranging pharmacological activities and presence of diverse natural products. Presently, green approaches to asymmetric Biginelli reaction are being explored for bioactive chiral DHPMs. In materials chemistry, DHPMs are increasingly finding applications in the development of materials such as polymers, adhesives, fabric dyes, etc. In view of the ease with which the Biginelli reaction is conducted, many exciting prospects await for its exploitation in various fields. (C) 2016 Elsevier Ltd. All rights reserved.

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