Recent advances in the regioselective synthesis of Pyrazoles

Joo Yong Yoon, Sang gi Lee, Hyunik Shin

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68 Scopus citations


Pyrazole is the ubiquitous sub-structure of many natural products and biologically active compounds. In this respect, its regioselective synthesis drew a lot of attention from synthetic organic chemists, leading to the development of various regioselective modifications of the classical Knorr cyclocondensation reaction and alternative methods. This review covers the period of 2003 to the middle of 2009 on the regioselective synthesis of pyrazoles, which are categorized into four reaction types: (i) modified Knorr condensation reaction using 1,3-dicarbonyl surrogates; (ii) 1,3-dipolar cycloadditions approach; (iii) regioselective direct substitution reaction of the pyrazole ring system; and (iv) other methods.

Original languageEnglish
Pages (from-to)657-674
Number of pages18
JournalCurrent Organic Chemistry
Issue number5
StatePublished - 2011


  • Pyrazole
  • Regioselective condensation
  • Regioselective cross-coupling
  • Regioselective dipolar cycloaddition


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