| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for selectivity producing an ethanesulfonylpiperidine derivative enantio-selectivity in a high yield without passing through an unstable intermediate. SOLUTION: This method for producing the ethanesulfonylpiperidine derivative having a stereo specific structure comprises reacting a protected amino acid ester with a 4-substituted butyric acid derivative in the presence of a base, then cyclizing, bezylating the obtained protected 3-oxopiperidine carboxylic acid alkyl salt, then decarboxylating in the presence of a strong acid, asymmetrically hydrogenating in the presence of a ruthenium complex containing a chiral disphosphine ligand and a chiral diamine, de-protecting the protection group (the order of the asymmetric hydrogenation and the de-protection can be reversed) and then reacting the de-protected product with a sulfone derivative. |
