Journal
TETRAHEDRON
Volume 65, Issue 44, Pages 8956-8960Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2009.06.104
Keywords
Cascade reaction; Coupling; 1,4-Benzoazepin-3-one; Heterocycles; Amino acids
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Funding
- Chinese Academy of Sciences
- National Natural Science Foundation of China [20621062, 20872156]
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CuI-catalyzed coupling of 2-bromobenzylamines and alpha-amino acids and subsequent condensative cyclization (directly or mediated with DPPA) provides 1,4-benzodiazepin-3-ones in moderate yields. Using L-proline and L-valine as the starting materials enantiopure products are obtained although partial racemization occurs for other amino acids. (C) 2009 Elsevier Ltd. All rights reserved.
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