A Cyclobutane possessing Hypotensive Activity

Abstract

A NUMBER of non-quaternary bases have been found to possess ganglionic blocking and hypotensive properties^1–5. In investigating the pharmacological properties of a new series of cyclobutanes⁶, one of them, 3-dimethylamino-2,2,4,4-tetramethyl-cyclobutanol, was found to exhibit a lowering activity of the blood pressure of long duration. The pharmacological properties of the cis isomer of this tertiary amine were qualitatively similar to those of the trans isomer. The cis isomer appeared, however, to be slightly less active when tested for hypotensive activity. Beard and Burger⁷ have recently reported the synthesis of the cis and trans isomers of 3-dimethylamino cyclo-butanol. They found the antispasmodic activity of the cis isomer of the diphenylacetic acid ester of 3-dimethylamino cyclobutanol to be slightly less than that of the trans isomer.