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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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Supplementary files

Article information


Submitted
12 Dec 2018
Accepted
21 Jan 2019
First published
22 Jan 2019

Org. Biomol. Chem., 2019,17, 1552-1557
Article type
Paper

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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