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US 2006/0069270 A1Published application
Process for the preparation of 1,3,5-trisubstituted pyrazoles via [3+2] cycloaddition
OwnerRafael Shapiro, Lucius Rossano +1inventors
InventorsRafael Shapiro, Lucius Rossano, Karen Tenhuisen
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Abstract
A process for the preparation of 1,3,5-trisubstituted pyrazole compounds, which are useful intermediates in the synthesis of factor Xa inhibitors.
Claims9
A process for preparing a compound of formula VI, or a pharmaceutically acceptably salt thereof,
- wherein D is 2-cyanophenyl, 2-(Pg-NHCH2)phenyl, 2-(aminomethyl)phenyl, 3-cyanophenyl, 3-(Pg-NHCH2)phenyl, 3-(aminomethyl)phenyl, 3-cyano-4-fluorophenyl, or (3-amino)benz[d]isoxazol-6-yl, in which Pg is an amine protecting group;
- and R is C1-C4 alkyl,
- comprising reacting a compound of formula IV,
- wherein X is Cl, Br, OMs, OSO2Ph, or OTs,
- with a compound of formula Vb in the presence of a base,
- wherein X1 is Br or Cl, and R is defined same as hereinabove.
3 more elements
Dependencies are inferred from the claim text.