Process for preparing 3-substituted indazoles
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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Abstract
The invention provides a method of preparing compounds of formula I and VIII: ##STR1## which are useful intermediates to compounds that are used as antagonists and partial agonists for the serotonin receptor 5-HT4.
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12 Claims
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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## - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- ##STR15## consisting of;
Specification