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Synthesis 2016; 48(24): 4580-4588
DOI: 10.1055/s-0035-1562618
DOI: 10.1055/s-0035-1562618
paper
Large-Scale Synthesis of Piperazine-2,6-dione and Its Use in the Synthesis of Dexrazoxane Analogues
Further Information
Publication History
Received: 07 June 2016
Accepted after revision: 22 July 2016
Publication Date:
31 August 2016 (online)
![](https://www.thieme-connect.de/media/synthesis/201624/lookinside/thumbnails/ss-2016-z0415-op_10-1055_s-0035-1562618-1.jpg)
Abstract
An efficient, large-scale synthesis of piperazine-2,6-dione was developed. The advantages of this procedure include the use of inexpensive starting materials, satisfactory yields, and a convenient workup without the need for chromatographic techniques. Furthermore, this procedure can be easily modified for the preparation of 1-substituted piperazine-2,6-dione hydrobromides. The utility of the prepared piperazine-2,6-dione was demonstrated in the synthesis of a novel analogue of the only drug used in clinical practice to prevent anthracycline-induced cardiotoxicity, dexrazoxane.
Key words
piperazine-2,6-dione - large-scale synthesis - dexrazoxane - cyclization - synthesis - formamideSupporting Information
- Supporting information for this article is available online at http://dx.doi.org/10.1055/s-0035-1562618.
- Supporting Information
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