Butyrophenones as hypotensive agents. Derivatives of 4 aryl 4 (hydroxymethyl)cyclohexylamine

Article abstract of DOI:10.1021/jm00240a014

The preparation of butyrophenone derivatives of 4 aryl 4 (hydroxymethyl) cyclohex 1 ylamines starting from the corresponding 4 cyano 4 phenylcyclohexan 1 ones is described. Substitution was varied in both rings; both isomers of 4 phenyl 4 (hydroxymethyl)cyclohex 1 ylamine were characterized. Those derivatives which carried p fluoro substitution on the butyrophenone exhibited hypotensive activity in the rat with diminished CNS activity compared to compounds lacking the hydroxymethyl group. The effect of substitution on the 4 aryl ring is discussed.