| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for manufacturing an optically active quaternaryα-amino acid without using an external chiral ligand or a chiral auxiliary group, which method attains high stereoselectivity in an alkylation reaction other than a methylation reaction. SOLUTION: An optically activeα-amino acid derivative which has a pseudo-enol structure and can form an intramolecular association (for example, 2-(2-hydroxyphenyl)-ethyl (2S)-2-(N-tert-butoxycarbonyl-N-methoxymethylamino)-3-phenylpropionate) is treated with a strong base at -30°C or below to form an enolate, which is reacted with an electrophilic agent: R<SP>2</SP>CH<SB>2</SB>X (wherein X is a leaving group such as chlorine, bromine, iodine or a p-toluenesulfonyl group). COPYRIGHT: (C)2004,JPO |
