| 摘要 |
<p>PURPOSE:To readily obtain the present substance in high purity and yield, by reacting a 3-halo-1-alkyl(or aryl)sulfonyloxy-2-propanol with an aromatic alcohol and aminating the resultant optically active glycidyl ether. CONSTITUTION:An (R)-alcohol or (S)-alcohol expressed by formula I (X is halogen; Y is aliphatic or aromatic residue) is reacted with an aromatic alcohol in the presence of a basic compound (preferably alkaline metal compound) in a hydrophilic organic solvent, such as DMSO, to provide an optically active glycidyl ether expressed by formula II (Ar is aromatic residue). The resultant compound without special isolation or purification thereof is then reacted with an aminating agent (e.g. isopropylamine) to afford the aimed compound expressed by formula III (R and R' are aliphatic residue). The aimed substance is obtained only in two steps from readily available raw materials of high optical purity according to the above-mentioned method. The present substance is useful as a drug for adult diseases, such as a drug for hypertension or arrhythmia.</p> |
