The Open Organic Chemistry Journal

2008, 2 : 92-99
Published online 2008 November 12. DOI: 10.2174/1874095200801020092
Publisher ID: TOOCJ-2-92

Solvent-Free Synthesis of Fused Pyrazolo[1,5-a]pyrimidines by Reaction of 5-Amino-1H-pyrazoles and β -Triketones

Jairo Quiroga , Jaime Portilla , Silvia Cruz , Rodrigo Abonía , Braulio Insuasty , Manuel Nogueras , Justo Cobo and Mike Hursthouse
Grupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A.A. 25360, Cali, Colombia and Grupo de Investigación en Compuestos Bio-orgánicos, Departamento de Química, Universidad de los Andes, Carrera 1 N° 18A 10, Bogotá, Colombia.

ABSTRACT

The solvent-free reaction between 5-amino-1H-pyrazoles and β-triketones (2-acetyldimedone and 2- acetylindandione) leads to the formation of new fused pyrazolo[1,5-a]pyrimidines in good yields. A possible mechanistic route is postulated on the basis of the isolation of the cyclization intermediate. The structures and regiospecificity of the reaction were determined on the basis of nmr measurements and X-ray diffraction.

Keywords:

5-Amino-1H-pyrazole, β-triketones, trimethyl ortho-acetate.