Novel spiro imidazoline compounds, their prepn. method and medicinal compsns. containing same
A compound, imidazoline ring technology, applied in the directions of the active ingredients of heterocyclic compounds, drug combinations, medical preparations containing active ingredients, etc., can solve the problems of long development time and other problems
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Embodiment 1
[0061] Spiro[(1,3-diazacyclopent-1-ene)-5,2'(S)-(trans-1',2',3',4',4'a(R),9 ', 9'a(S), 10'-octahydroanthracene)] fumarate
[0062] and spiro[(1,3-diazacyclopent-1-ene)-5,2'(R)-(trans-1',2',3',4',4'a(S), 9',9'a(R),10'-octahydroanthracene)] fumarate
[0063] Step 1: 7-(2-Bromobenzyl)-1,4-dioxaspiro[4.5]decan-8-one
[0064] Under a nitrogen atmosphere, a THF (360ml) solution of 1,4-cyclohexanedione monoethylene glycol (20g, 28mmol) was added dropwise to a 1M THF solution of lithium diisopropylamide cooled to -78°C (150mmol, 150ml), then, the mixture was allowed to warm to room temperature, and after stirring for 1 hour, the mixture was cooled to -78°C and 35.2g (141mmol) of 2-bromobenzyl bromide was added dropwise. After stirring at -78°C for 30 minutes, the temperature of the mixture was allowed to rise to 0°C. The mixture was stirred at 0°C for 3 hours, then hydrolyzed and the mixture was extracted with ether. The organic phase was washed with saturated NaCl solution, wash...
Embodiment 2
[0096] Spiro[(1,3-diazacyclopent-1-ene)-5,2'(S)-(trans-1',2',3',4',4'a(S),9 ', 9'a(R), 10'-octahydroanthracene)] fumarate and
[0097] Spiro[(1,3-diazacyclopent-1-ene)-5,2'(R)-(trans-1',2',3',4',4'a(R),9 ', 9'a(S), 10'-octahydroanthracene)] fumarate
[0098] from (2S)-2-Aminomethyl-trans-1,2,3,4,4a(S), 9,9a(R), 10-octahydro-2-anthracenamine and its enantiomers are carried out according to Example 1 step 7 method preparation.
[0099] Melting point: 215°C.
[0100] pharmacological research
Embodiment A
[0101] Example A: Determination of α2-adrenergic receptor affinity in rats
[0102] pass[ 3H]-RX821,002 competition assay to determine affinity. Membranes were prepared from rat cerebral cortex and treated with 0.4nM[ 3 H]-RX821,002 and the compound to be tested were incubated in triplicate at 22°C for 60 minutes in a final volume of 1.0 ml. The incubation buffer contained 50 nM TRIS-HCl (pH 7.5), 1 mM EDTA and 100 μM GppNHp. Non-specific binding was determined with 10 [mu]M phentolamine.
[0103] data analysis
[0104] At the end of the incubation, the incubation medium was filtered through WHATMAN GF / B filters soaked with 0.1% polyethyleneimine and washed three times with 5 ml of cold buffer. The radioactivity retained on the filters was measured by liquid scintillation counter and binding isotherms were analyzed by nonlinear regression.
[0105] result
[0106] The compounds of the present invention exhibit specific α2-adrenoceptor antagonist activity, for example ...
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