PROCESS FOR PRODUCING BENZODIAZEPIN DERIVATIVES

摘要

Cpds. of formula (I): where R1 = halogen; R2 = H or lower alkyl; R3 = H or halogen; n = 1 or 2; including acid-addn. salts; are prepd. by reacting a cpd. (II): with opt. protected cpd. (III): - protecting groups where R4 and R5 = H or an easily removable protecting group. (I) have sedative-, muscle-relaxant and anticonvulsive action of the same order as known benzodiazepins, and are strongly hydrophilic and better suitable for the prepn. of mainly injection solns. Pref. cpd. (I) is 7-chloro (2,3-dihydroxypropyl)5-(2-fluorophenyl)-1,3-dihydro 2H 1,4-benzodiazepin-2-one.