| 摘要 |
<p>PROBLEM TO BE SOLVED: To efficiently obtain the subject compound useful as an intermediate for bestatin as an anticancer agent in high yield by treating a specific diastereomer in the presence of an amine and an organic solvent. SOLUTION: This optically active cyanohydrin of the formula (R<1> and R<2> are each H or an amino-protecting group; the configuration of *2 and *3 are such one that, when *2 stands at R-configuration, *3 stands at S- configuration, and vise versa) is obtained by treating (A) a diastereomer mixture of N-(protected)-3-amino-2-hydroxy-4-phenylbutyronitrile in the presence of (B) an amine (pref. tertiary amine, esp. triethylamine) and (C) an organic solvent such as ether-based solvent, aliphatic hydrocarbon-based solvent or aromatic hydrocarbon-based solvent. The amount of the component B to be used is pref. 0.1-10mol% based on the component A. The temperature during the treatment is pref. 0 deg.C to the reflux temperature. In the component C, the ether-based solvent is pref. isopropyl ether, the aliphatic hydrocarbon-based solvent pref. n-heptane, and the aromatic hydrocarbon-based solvent pref. toluene.</p> |
