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Aqueous N-Heterocyclization of Primary Amines and Hydrazines with Dihalides: Microwave-Assisted Syntheses of N-Azacycloalkanes, Isoindole, Pyrazole, Pyrazolidine, and Phthalazine Derivatives

Yuhong Ju and Rajender S. Varma*

*Clean Processes Branch, Sustainable Technology Division, National Risk Management Research Laboratory, U.S. Environmental Protection Agency, 26 West Martin Luther King Drive, MS 443, Cincinnati, Ohio 45268, Email:

Y. Ju, R. S. Varma, J. Org. Chem., 2006, 71, 135-141.

DOI: 10.1021/jo051878h (free Supporting Information)

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A one-pot synthesis of nitrogen-containing heterocycles from alkyl dihalides and primary amines and hydrazines occurs under microwave irradiation via a simple and efficient cyclocondensation in an alkaline aqueous medium.

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Key Words

Cyclic Amines, Azetidines, Pyrrolidines, Piperidines, Pyrazolines, N-Heterocycles, Microwave Synthesis, Green Chemistry

ID: J42-Y2006-2770