A new series of tricyclic (aryloximino)propanolamines displaying very high selective .beta.2-blocking properties
作者:Brigitte Jamart-Gregoire、Paul Caubere、Marie Blanc、Jean Pierre Gnassounou、Charles Advenier
DOI:10.1021/jm00122a008
日期:1989.2
A new class of indanones 4 easily obtained by aryne type condensations, followed by transposition of the benzocyclobutanols 3 thus formed, were transformed into the corresponding oximinopropanolamines 7. These compounds were studied for their potential beta-blocking properties. It was found that 7 have generally low beta 1-blocking properties. Their beta 2-blocking action varies from low to very high
It is shown that benzocyclobutenols are excellent starting materials for the obtention of polycyclic aromatic ketones. Thus under basic conditions they lead to benzocyclenedione mono ketals which may be hydrolyzed into the corresponding benzocyclenediones. Under acidic conditions, a transposition takes place leading to indanone derivatives. The mechanism of this transposition is discussed.