1,4-benzodiazepines prepn

摘要

of formula (I) (where R1=H, Me, Et, Pr or cyclopropyl, and R2 =H, halo, NO2, or CH2F, are prepd by an improved method consisting of self-condensation of a 2-(2-haloacetamido)-5-substd benzophenone. in the presence of (CH2)6N4. The reactions is carried out in EtOH opt. contng. HCl and up to 15% H2O, above 50 degrees. The intermediate (CH2)6N4 salt may be isolated. (I) are sedatives and hypnotics.