期刊
TETRAHEDRON
卷 66, 期 31, 页码 5811-5818出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2010.05.080
关键词
Hypervalent iodine; Alkynylamides; PIFA; Reductive amination; Diazepines
资金
- University of the Basque Country [UPV 41.310-13656]
- Basque Government [GIU 06/87]
- Spanish Ministry of Science and Innovation [CTQ2007-64501/BQU]
The addition of the hypervalent iodine reagent PIFA [phenyliodine(III) bis(trifluoroacetate)] to a series of properly substituted N-(3-aminopropyl)alkynylamides results in the efficient formation of a functionalized 5-aroyl-2-pyrrolidinone skeleton. By proper manipulations of the N(1)-substituents, through consecutive deprotection and/or reductive amination steps, a second cyclization process occurs yielding the target heterocycles. As it will be disclosed, the overall process is open to structural modifications that gives rise to a series of pyrrolo(benzo)diazepine derivatives. (C) 2010 Elsevier Ltd. All rights reserved.
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