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Sci. Pharm. 2014, 82(3), 501-518; doi:10.3797/scipharm.1401-19

Short and Efficient Synthesis of Alkyl- and Aryl-Ortho-Hydroxy-Anilides and their Antibiotic Activity

Department of Pharmacy – Center for Drug Research, Ludwig-Maximilian-University, Butenandtstr. 5–13, 81377 Munich, Germany
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Received: 23 January 2014 / Accepted: 13 March 2014 / Published: 13 March 2014
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Abstract

Ortho-hydroxy-anilides are part of natural products like the new antibiotics platencin (A) and platensimycin (B). An important step in the total synthesis of these antibiotics or their derivatives is the preparation of the o-hydroxy-anilide partial structure. The presented method allows the preparation of o-hydroxy-anilides and o-dihydroxy-anilides from 2-nitrophenol esters in a one-step synthesis without protecting the hydroxy group. Aryl- and alkyl-anilides were prepared following this method as simple analogues of platensimycin (A). The resulting compounds were tested in an agar diffusion assay for their antibiotic potency.
Keywords: Anilides; Hydrogenation; Antibiotic activity; Aminolysis Anilides; Hydrogenation; Antibiotic activity; Aminolysis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

KRAUß, J.; PLESCH, E.; CLAUSEN, S.; BRACHER, F. Short and Efficient Synthesis of Alkyl- and Aryl-Ortho-Hydroxy-Anilides and their Antibiotic Activity. Sci. Pharm. 2014, 82, 501-518.

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