Chiral amino acids: A versatile tool in the synthesis of pharmaceuticals and fine chemicals

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Abstract

Methods of preparing enantiomerically pure amino acids especially focusing on amino-acylase-based resolution of D,L-acetylamino-acid precursors, synthesis of D-amino acids using a hydantoinase system, and the cofactor-dependent enzymatic reductive amination of α-keto acids to L-amino acids are described. Examples are given for bulk actives, based on L-and D-amino acids and peptides. L-and D-Tle (= L-/D-2-amino-3,3-dimethylbutanoic acid) are important molecules for synthesizing drugs and a great variety of chiral auxiliaries. A new chromatographic separation of bulky-side-chain amino acids in a preparative scale is described, giving both enantiomers in > 99% ee.

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Drauz, K. (1997). Chiral amino acids: A versatile tool in the synthesis of pharmaceuticals and fine chemicals. Chimia, 51(6), 310–314. https://doi.org/10.2533/chimia.1997.310

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