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

Monica Viviano; Ciro Milite; Donatella Rescigno; Sabrina Castellano; Gianluca Sbardella

doi:10.1039/C4RA13392G

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

Monica Viviano,^a Ciro Milite,^a Donatella Rescigno,^a Sabrina Castellano*^a and Gianluca Sbardella^a

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* Corresponding authors

^a Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy
E-mail: scastellano@unisa.it

Abstract

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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Publication details

The article was received on 29 Oct 2014, accepted on 27 Nov 2014 and first published on 27 Nov 2014

Article type: Paper

DOI: 10.1039/C4RA13392G

Citation: RSC Adv., 2015,5, 1268-1273

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

M. Viviano, C. Milite, D. Rescigno, S. Castellano and G. Sbardella, RSC Adv., 2015, 5, 1268
DOI: 10.1039/C4RA13392G
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Monica Viviano
Ciro Milite
Donatella Rescigno
Sabrina Castellano
Gianluca Sbardella

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

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

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