| 摘要 |
<p>PURPOSE:To prepare the titled compound useful as a beta-adrenergic neuronal blocking agent, in high yield, by using novel 3-(benzylisopropylamino)-2-benzyloxypropanol-1 and dicyclohexyl carbodiimide as raw materials through a novel intermediate, etc. CONSTITUTION:3-(Benzylisopropylamino)-2-benzyloxypropanol-1 of formulaI (novel compound) is made to react with dicyclohexyl carbodiimide to obtain the compound of formula II, which is reacted with 2-hydroxy-6-nitrotoluene to afford the novel compound of formula III. Reaction of the compound with bis(dialkylamino)- t-butoxymethane gives the novel compound of formula IV, which is converted to the compound of formula V by the catalytic reductive cyclization with hydrogen using platinum oxide catalyst, etc. The objective compound of formula VI can be obtained by the hydrolysis of the compound of formula V. Epichlorohydrin is not used as the raw material.</p> |
