微波辅助串联反应合成杂环
2009-03-16 15:09
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资料摘要:
Mohammed Abid, abid@bwh.harvard.edu, Department of Radioloy, Conjugate and Medicinal Chemistry Laboratory, Harvard Medical School, 75 Francis Street, Boston, MA 02115, Bela Torok, bela.torok@umb.edu, Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Blvd., Boston, MA 02125, and Xudong Huang, xhuang3@partners.org, Department of Radioloy, Brigham and Womens Hospital, Conjugate and Medicinal Chemistry Laboratory, Harvard Medical School, 75 Francis Street, Boston, MA 02115.
Nitrogen-containing heterocycles are of exceptional interest in pharmaceutical applications as they are pharmacorephores of several drugs, potential therapeutics and molecular imaging agents for neurological disorders, such as Alzheimer's disease. Due to strengthening environmental regulations and heightening safety concerns, the development of new environmentally favorable synthetic schemes are highly desirable. We have developed various environmentally benign methods for the synthesis of N-heterocycles and their derivatives utilizing microwave-assisted solid acid (montmorillonite K-10) catalysis. Herein we have reviewed our recent efforts on the development of microwave-assisted green synthetic technologies.
This strategy has enabled us to synthesize a wide range of N-heterocycles, such as pyrroles, indoles and carbazoles. This technique has been further perfected using the combination of K-10/Pd/C bifunctional catalyst and microwave irradiation to achieve the one-pot synthesis of pyrazoles, pyridine derivatives (Hantzsch synthesis) β-carbolines (modified Pictet-Spengler synthesis).
This work is supported by a research grant from the Alzheimer's Association (to XH).
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