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US 6,642,390 B2Granted
One step synthesis of 1,2,3-triazole carboxylic acids
AssigneeLexicon Pharmaceuticals, Inc.
InventorsHartmuth C. Kolb, Cullen Cavallaro, Zhi-Cai Shi, Alexander Gontcharov, Zhi-Min Wang, Paul F. Richardson, Ramanaiah C. Kanamarlapudi
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Abstract
Disclosed is a one step method for preparing a 1,2,3-triazole carboxylic acid by treating an azide with a β-ketoester in the presence of a base.
Claims13
A method for preparing a 3H-[1,2,3]-triazole-4-carboxylic acid comprising treating an azide with a β-ketoester in the presence of a base.
A method of preparing a 1,2,3-triazole of the formula
- wherein
- R1 and R2 independently are lower alkyl or cycloalkyl optionally substituted with one, two or three groups independently selected from halogen, lower alkoxy, —C(O)-alkyl, hydroxy, amino, mono- or dialkylamino, mercapto, alkylthiol, —C(O)NH-alkyl, C(O)N-dialkyl, alkenyl or alkynyl, or
- R1 and R2 independently are aryl, arylalkyl, heteroaryl or heteroarylalkyl wherein the ring portion of each is optionally substituted with one, two or three groups independently selected from halogen, lower alkoxy, —C(O)-alkyl, hydroxy, amino, mono- or dialkylamino, mercapto, alkylthiol, —C(O)NH-alkyl, C(O)N-dialkyl, alkenyl or alkynyl;
- the method comprising
- treating an azide of the formula
- with a β-ketoester of the formula
- wherein R3 is lower alkyl,
- in the presence of a base.
5 more elements
Dependencies are inferred from the claim text.