发明名称 |
Process for producing optically active azetidine-2-carboxylic acid |
摘要 |
The present invention provides an efficient, simple, and commercially advantageous process for producing optically active azetidine-2-carboxylic acid, which is an important material for medicines. The process includes the steps of halogenating an optically active N-protected 4-amino-2-hydroxybutyric acid following inversion of the configuration to produce an optically active N-protected 4-amino-2-halobutyryl halide; hydrolyzing the halide; deprotecting the amino group of the hydrolyzed product to produce an optically active 4-amino-2-halobutyric acid; cyclizing the product in an alkaline aqueous solution; and then protecting the amino group of the cyclized product to produce an optically active N-protected azetidine-2-carboxylic acid. The present invention also provides an optically active N-protected 4-amino-2-halobutyryl halide represented by general formula (2): (wherein P represents a protective group for the primary amino group; * indicates that the carbon atom is asymmetric; and each of X and Y independently represents a halogen atom), which is useful for producing the optically active azetidine-2-carboxylic acid.
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申请公布号 |
US2004171849(A1) |
申请公布日期 |
2004.09.02 |
申请号 |
US20040483628 |
申请日期 |
2004.01.14 |
申请人 |
KONDO TAKESHI;UEYAMA NOBORU |
发明人 |
KONDO TAKESHI;UEYAMA NOBORU |
分类号 |
C07C227/32;C07D205/04;C07D209/48;(IPC1-7):C07C229/02 |
主分类号 |
C07C227/32 |
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