C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/239.3
C07D 487/04 (2006.01) C07D 249/08 (2006.01) C07D 521/00 (2006.01)
Patent
CA 1043785
ABSTRACT OF THE DISCLOSURE A multi-step process for the preparation of 1-[(amino- or substituted amino)methyl]-6-phenyl-4H-s-triazolo- [4,3-a][1,4]benzodiazepines of the formula VI: Image VI wherein R' is hydrogen or alkyl of 1 to 3 carbon atoms, inclusive, and wherein the rings A and B are unsubstituted or substituted by one or two substituents selected from the group consisting of chloro, fluoro, bromo, nitro, and tri- fluoromethyl, which comprises: treating a compound of the formula I: Image I wherein rings A and B are defined as above, with acetic anhydride and formic acid to obtain compound II: -1- Image II wherein A and B rings have the significance as above, treating compound II with sufficient formaldehyde to produce compound III, the 3,5-bis(hydroxymethyl)derivative of II; treating III with phthallmide, triphenylphoshine and diethyl azodicarboxylate to give compound IV, the 3,5-bis(phthalimidomethyl) derivative of II; and treating IV with hydrazine hydrate to obtain a compound of formula V Image V wherein rings A and B are defined, as herein above. Com- pound V can then be alkylated in know manner to give those compounds of formula VIa which comrresponds to formula VI when R' is desired to be alkyl. The compounds of formula VI have antidepressant and antianxiety effects in mammals and birds. -Ib-
227603
Gall Martin
Hester Jackson B. (jr.)
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