4.6 Article

A continuous-flow synthesis of 1,4-benzodiazepin-5-ones, privileged scaffolds for drug discovery

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RSC ADVANCES
卷 5, 期 2, 页码 1268-1273

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ra13392g

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  1. Italian Ministero dell'Istruzione, dell'Universita e della Ricerca (MIUR)-Progetti di Ricerca di Interesse Nazionale [PRIN 20103W4779, PRIN 2012ZHN9YH]
  2. Universita di Salerno (Italy)
  3. Universita a di Salerno

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An efficient and gram-scale continuous-flow protocol for the synthesis of the privileged structure 3,4-dihydro-5H-benzo[e][1,4]diazepin-5-one is reported. If compared to the traditional metal mediated non-catalytic reduction procedure, this approach is high yielding and does not require purification steps and therefore could be conveniently used for the generation of compound libraries for drug discovery.

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