1246513-85-8Relevant academic research and scientific papers
Process for preparing chiral β-amino acid derivative by asymmetric hydrogenation with cinchona-derived organocatalyst
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, (2017/10/10)
The present invention provides a production method of a chiral beta-amino acid derivative by an asymmetric hydrogenation reaction using a cinchona-derived organic catalyst. The production method of a chiral beta-amino acid derivative of the present invention can be used as a production method of a chiral compound, and a method synthesizing an optically high-purity compound in an ezetimibe synthesis field.COPYRIGHT KIPO 2017
Efficient preparation of an N-aryl β-amino acid via asymmetric hydrogenation and direct asymmetric reductive amination en route to Ezetimibe
Busscher, Guuske F.,Lefort, Laurent,Cremers, Jozef G.O.,Mottinelli, Marco,Wiertz, Roel W.,Lange, Ben De,Okamura, Yutaka,Yusa, Yukinori,Matsumura, Kazuhiko,Shimizu, Hideo,De Vries, Johannes G.,De Vries, Andre H.M.
experimental part, p. 1709 - 1714 (2010/10/20)
Two routes for the preparation of an N-aryl β-amino acid, an important precursor for the cholesterol-lowering drug Ezetimibe, were investigated. The first pathway proceeds via an Rh- or Ir-catalyzed asymmetric hydrogenation of N-aryl enamine giving the desired product with up to 82% ee. The other pathway involves a direct asymmetric reductive amination (DARA) of the β-keto ester which yielded the β-amino ester in high yield and 97% ee. Subsequent copper-catalyzed N-arylation gave the target compound.
NOVEL N-SUBSTITUTED BETA-AMINO ACID ESTERS
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Page/Page column 12-13, (2010/04/03)
The present invention relates to β-amino acid esters of Formula (2), and to a method for the preparation of β-amino acid esters of formula (2) by reduction of the corresponding enamines or amination of a β-keto ester followed by condensation with a halogen-substituted benzene derivative.
