METHOD OF SYNTHESIS OF TRIAZOLO-[4,3-A]-[1,4]-DIAZEPINES Russian patent published in 1997 - IPC

FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: product: triazolo-[4,3-a]-[1,4]-diazepines of the general formula (I) where X - radical: -CH=CH- or S; R¹ - lower alkyl or trifluoromethyl; R² - chlorine or fluorine; R³ - radical: R⁴-(CH₂)_n-C-triple bond-C or R⁵-O-CH₂-C-triple bond-C; R⁴ - phenyl or mono-, di- or tricyclic 5-7-membered heterocyclic radical containing oxygen or sulfur and/or 1-3 nitrogen atoms as heteroatoms that can be free or substituted with lower alkoxy, oxo, hydroxy-group or chlorine; R⁵ - phenyl or pyridyl. Reagent 1: the corresponding (R³)-unsubstituted triazolo-[4,3-a]-[1,4]-diazepine. Reagent 2: Z-substituted acetylene where Z - radical of the formula: R-(CH₂)_n- or R⁵-O-CH₂. Reaction conditions: in medium of inert solvent, at temperature from the room one to about 100 C, in the presence of palladium catalyst. Synthesized compound show PAF-antagonistic action. EFFECT: improved method of synthesis. 2 tbl