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Synthesis 1999; 1999(4): 588-592
DOI: 10.1055/s-1999-3431
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A Versatile and Efficient Synthesis of Substituted 1H-Indazoles

Stéphane Caron* , Enrique Vazquez
  • *Process Research and Development, Central Research Division, Pfizer Inc., Eastern Point Road, Groton, Connecticut 06340, USA; Fax +1(8 60)4 41-36 30; E-mail: stephane_caron@groton.pfizer.com
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Publication Date:
31 December 1999 (online)

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A facile synthesis of substituted 1H-indazole 4 from aryl mesylate 3 is described. The reaction, which proceeds through the intermediate hydrazone, was general with regard to the substituents on the arene and was applicable to several hydrazines. It was also discovered that with p-methoxyphenylhydrazine, the indazole formation was more rapid than the competitive Fischer indole synthesis.

1H-indazole - phenol - mesylate - hydrazine - hydrazone