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Paper | Regular issue | Vol 60, No. 11, 2003, pp.2499-2510
Published online, 5th September, 2003
DOI: 10.3987/COM-03-9869
Synthesis of Multi-substituted Pyrazoles Utilizing the N-Alkylated 3-Hydroxy-3-propargyl- or Allenylisoindolines

Yong Hyun Choi, Kyung Soon Kim, Sangku Lee, Tae-Sook Jeong, Hee-Yoon Lee, Yong Hae Kim, and Woo Song Lee*

*Korea Research Institute of Bioscience and Biotechnology, 52 Oun, Yusong, Daejeon 305-333, Korea


N-Alkyl-substituted phthalimides (1) were easily converted to di-, tri-, and tetra-substituted pyrazoles (10) via a one-pot addition-decyclization-cyclocondensation process. Then, the structure and the position of N1-substitution of the 1,3-pyrazole ring were determined by X-Ray crystallographic analysis and 1H-nOe experiments.