| abstract |
The present invention provides an optically active 3-amino-2-hydroxypropionic acid cyclopropylamide derivative useful as a pharmaceutical intermediate or a salt thereof, which can be easily produced from inexpensive and readily available raw materials, and is practical for industrial production. It is an object of the present invention to provide a practical method and useful intermediates thereof. This problem is solved by the following method. First, an easily available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced and then epoxidized to produce an optically active epoxycarboxylic acid derivative. Next, it is reacted with cyclopropylamine to convert to an optically active epoxyamide derivative, and then reacted with nitrile to produce an optically active oxazolineamide derivative. Subsequently, an optically active 3-amino-2-hydroxypropionic acid cyclopropylamide derivative or a salt thereof is produced by selective acid solvolysis of the oxazoline skeleton. [Selection figure] None |