Isoxazoles. XVIII. Synthesis and Pharmacological Properties of 5-Aminoalkyl- and 3-Aminoalkylisoxazoles and Related Derivatives.

A number of 3-substituted 5-aminoalkyland 5-substituted 3-aminoalkylisoxazoles and some related amino alcohols have been prepared for pharmacological testings. Besides ordinary transformations of the corresponding alcohols and acetyl derivatives to the aminoalkyl derivatives and amino alcohols, a convenient synthetic method for the 5-aminoalkyl series which involves 1,3-dipolar cycloaddition of nitrile oxides to aminoalkynes has been developed. Several of the compounds proved to exhibit a wide spectrum of pharmacological propertier wrhic.h incaliide potent hypothermic, analgesic, antiinflammatory, a i ~ d ant itiisqive activities.