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Process for preparing 3-substituted indazoles

  • US 5,914,405 A
  • Filed: 09/30/1998
  • Issued: 06/22/1999
  • Est. Priority Date: 10/07/1997
  • Status: Expired due to Fees
First Claim
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1. A process for preparing a compound of the formula:

  • ##STR15## consisting of;

    a) oxidizing a compound of formula VII(a);

    ##STR16## by heating a mixture of a compound of formula VII(a), a substituted benzene solvent, and an oxidation catalyst at a temperature between 110°

    C. and the reflux temperature of the mixture to form a compound of formula I(a);

    ##STR17## b) optionally filtering the resulting reaction mixture from step a);

    c) adding a suitable base to the resulting reaction mixture of step a) or to the filtrate of step b) to form a compound of the formula VIII(a);

    ##STR18## d) optionally reacting the compound of formula VIII(a) with a carbonyl activating reagent to provide a compound of the formula;

    ##STR19## wherein R12 is a carbonyl activating group; and

    e) reacting the compound of formula VIII(a) or the compound of formula XI(a) with an amine of the formula ##STR20##

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