| 摘要 |
<p>PREPARATION OF AROMATIC KETONES HAVING CARDIOVASCULAR ACTIVITY Compounds of the formula: in which R1 and R2 each is an alkyl group having 1 to 4 carbon atoms and R4 is a halogen atom having therapeutic value in the treatment of cardiovascular conditions are formed by reacting a substituted salicylic aldehyde of the formula: with a 1-alkylamino-2-hydroxy-3-chloropropane of the formula: C1CH2.CHOH.CH2NHR in an anhydrous solvent in the presence of a dehydrating agent, treating the resulting 3-alkyl-5-chloromethyl-2- (orthohydroxyphenyl)oxazolidine in a dipolar aprotic solvent with a basic agent to produce an 8-aza-4,9-dioxa-2,3-benzo-¢4,2,1!-bicyclooctane, subjecting the latter material to acid hydrolysis to produce a 2-(3-alkyl-amino-2-hydroxypropoxy) benzaldehyde, reducing the benzaldehyde to the corresponding benzyl alcohol and oxidizing the benzyl alcohol with chromic acid in the presence of sulphuric acid.</p> |
