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Paper | Regular issue | Vol 68, No. 10, 2006, pp.2063-2077
Published online, 25th August, 2006
DOI: 10.3987/COM-06-10824
Synthesis of Novel Pyrazolopyrrolizinones as Prospective Anticancer Agents

Christophe Rochais, Jana Sopkovà-de Oliveira Santos, Patrick Dallemagne, and Sylvain Rault*

*CERMN, Faculty of Pharmacy, 1, rue Vaubénard, 14032 Caen Cedex, France


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 N-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.