SYNTHESIS OF NOVEL PYRAZOLOPYRROLIZINONES AS PROSPECTIVE ANTICANCER AGENTS

摘要

Herein we describe the access of novel pyrazolopyrrolizinones from commercial arylacetonitriles. The first step conducts to the corresponding aminoester which was first submitted to Clauson-Kaas procedure. Amidification and cyclisation afford then the first examples of the expected heterocycles. In order to improve the sequence and to obtain N-substituted isomers, 3-aryl-5-(pyrrolidin-1-ylcarbonyl)-4-(1H-pyrrol-1-yl)-1H-pyrazoles (5) were alkylated and conduct to two different TV-substituted pyrazoles. These novel products were separated by chromatography and clearly identified using different analytical techniques. Application of the cyclisation procedure conducts then to the two corresponding final title products.