<br/>Pirazolines and pirazolidines are a very important class of five-membered, nitrogen-containing heterocycles. These pharmacophores are essential for the biological properties of many drugs and natural products. Thus, there is a continuous demand for the development of more efficient and systematic methods to access these key scaffolds. We have found an efficient and convergent method for the synthesis and isolation of Cbz and Boc protected diaziridine synthons. These molecules have shown to undergo cycloaddition reactions with alkynes and alkenes across the C-N bond in the presence of a transtion-metal catalyst to form pyrazolines and pyrazolidines. This study would provide reliable and selective route towards the synthesis of highly functionalized pyrazolines, pyrazoldines and more complex cycloaddition adducts.

Diastereoselective dipolar cycloadditions for the synthesis of pyrazoline and pyrazolidine pharmacophores

249th National Meeting (2015)

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