2-(2-(hydroxymethyl)-imidazo-1-yl)benzophenones

C - Chemistry – Metallurgy – 07 – D

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260/315.25

C07D 233/64 (2006.01) C07D 233/54 (2006.01) C07D 487/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 1059522

ABSTRACT OF THE DISCLOSURE Compounds of formula II Image II and its phthalimide derivative III: Image III wherein R0 and R1 are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive, wherein R2 is hydrogen, chloro, fluoro, or trifluoromethyl; wherein R3 is hydrogen, or fluoro with the proviso that R3 is not fluoro, if R2 is chloro or trifluoromethyl; and wherein R4 is hydrogen, fluoro, chloro, bromo, nitro, or trifluoromethyl are prepared by reacting a compound of formula I: -1- Image I wherein R0, R1, R2, R3, and R4. are defined as above, with formaldehyde to produce compound II and reacting II with phthalimide, triphenylphosphine and finally diethyl azo- dicarboxylate to give compound III. Compounds II and III are useful as important inter- mediates for the production of known 6-phenyl-4H-imidazo- [1,2-a][1,4]benzodiazepine which compounds are active as tranquilizers and antianxiety agents. -1a-

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