Process for the manufacture of diazepine derivatives

Details Process for the manufacture of diazepine derivatives Process for the manufacture of diazepine derivatives

C - Chemistry, Metallurgy

07

D

260/239.4

C07D 487/04 (2006.01) C07D 495/14 (2006.01) C07F 9/6533 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 1090333

ABSTRACT Imidazodiazepine derivatives of the formula Image I wherein Image represents the group Image Image or Image a b c A represents the group Image or Image , R represents hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl or lower alkanoyl, R1 represents hydrogen, chlorine, bromine or iodine, R2 represents hydrogen or lower alkyl, R3 represents phenyl, mono-sustituted phenyl, disubstituted phenyl, pyridyl or mono-substituted pyridyl, R4 represent lower alkyl and n represents the integer 0 or 1, are prepared by a novel process which comprises reacting compound of the formula Image II wherein Image , A and R2 have the meaning indiated above and Y represents a suitable leaving group, with an isocyanoacetate of the formula C?N-CH2-COOR4 III wherein R4 has the meaning indicated above, in the presence of a base strong enough to generate the anion of the isocyanoacetate. The compounds of the formula I are in part novel and in part known and are useful as muscle relaxants, sedatives, anxiolytics and anti-convulsants.

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