5-(2-Fluorophenyl)-7-iodo-1,3-dihydro-2H-1,4-benzodiazepine - prepd. by ring-enlargement of hydroxy- and carboxy-substd. quinolines

摘要

Benzodiazepines of formula (I) (where R1 is H or CH3) and their acid addn salts are prepd by subjecting quinolines of formula (II) (where R2 is lower alkyl) to ring-enlargement and acidic hydrolysis (with dehydration) under aqs. conditions and to decarboxylation. (I) are sedatives, muscle relaxants and anticonvulsants, e.g. (I; R1=CH3) has an ED50 of 1.6 mg/kg in the maximal electroshock.