An efficient one-pot, two-step synthesis of 4-substituted 1-heteroarylpiperazines under microwave irradiation conditions |
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| Authors: | Hong-Jun Wang William G. Earley Robert M. Lewis Rajiv R. Srivastava Andrew J. Zych David M. Jenkins David J. Fairfax |
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| Affiliation: | Department of Medicinal Chemistry, Albany Molecular Research, Inc., PO Box 15098, 21 Corporate Circle, Albany, NY 12212-5098, USA |
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| Abstract: | A highly efficient one-pot, two-step microwave procedure has been developed for the synthesis of 4-substituted 1-heteroarylpiperazines. Microwave heating of heteroaryl chlorides with 1,4-diazabicyclo[2.2.2]octane (DABCO) at 160 °C for 15 min yielded 1-heteroaryl-4-(2-chloroethyl)piperazines, which could be further reacted with various nucleophiles, again under microwave irradiation conditions, to give an array of 4-substituted 1-heteroarylpiperazines in good to excellent yields. |
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| Keywords: | Dealkylation Heteroaryl DABCO Piperazine Microwave irradiation |
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