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Issue 6, 2019
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Continuous-flow protocol for the synthesis of enantiomerically pure intermediates of anti epilepsy and anti tuberculosis active pharmaceutical ingredients

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Abstract

Continuous-flow production of chiral intermediates plays an important role in the development of building blocks for Active Pharmaceutical Ingredients (APIs), being α-amino acids and their derivatives widely applied as building blocks. In this work we developed two different strategies for the synthesis of intermediates used on the synthesis of levetiracetam/brivaracetam and ethambutol. The results obtained show that methionine methyl ester can be continuously converted to the desired ethambutol intermediate by RANEY® Nickel dessulfurization/reduction strategy whereas levetiracetam/brivaracetam intermediates could be synthesized by both RANEY® Nickel (without H2) and Pd/C–H2 approach or by photochemical desulfurization.

Graphical abstract: Continuous-flow protocol for the synthesis of enantiomerically pure intermediates of anti epilepsy and anti tuberculosis active pharmaceutical ingredients

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Publication details

The article was received on 12 Dec 2018, accepted on 21 Jan 2019 and first published on 22 Jan 2019


Article type: Paper
DOI: 10.1039/C8OB03088J
Citation: Org. Biomol. Chem., 2019,17, 1552-1557

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    Continuous-flow protocol for the synthesis of enantiomerically pure intermediates of anti epilepsy and anti tuberculosis active pharmaceutical ingredients

    R. M. Aguiar, R. A. C. Leão, A. Mata, D. Cantillo, C. O. Kappe, L. S. M. Miranda and R. O. M. A. de Souza, Org. Biomol. Chem., 2019, 17, 1552
    DOI: 10.1039/C8OB03088J

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