Facile synthesis of 1,4-benzodiazepin-3-ones from o-bromobenzylamines and amino acids via a cascade coupling/condensation process |
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| Authors: | Hexiang Wang Kun Gao Dawei Ma |
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| Affiliation: | a State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China
b State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China |
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| Abstract: | CuI-catalyzed coupling of 2-bromobenzylamines and α-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. |
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| Keywords: | Cascade reaction Coupling 1,4-Benzoazepin-3-one Heterocycles Amino acids |
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