【药物名称】Medetomidine, MPV-785(hydrochloride), Domitor
化学结构式(Chemical Structure):
参考文献No.2435
标题:Antihypertensive subtituted imidazole derivates
作者:Karjalainen, A.J.; Kurkela, K.O.A.; Pohjala, E.K. (Orion Pharma)
来源:GB 2101114; US 4639464
合成路线图解说明:

The Grignard condensation of methyl imidazole-4-carboxyate (I) with 2,3-dimethylphenylmagnesium bromide (II) in THF gives 4-(2,3-dimethylbenzoyl) imidazole (III), which (without isolation) is submitted to a new Grignard condensation with methylmagnesium iodide (IV) in the same solvent to yield 1-(4-imidazolyl)-1-(2,3-dimethylphenyl)ethanol (V). The dehydration of (V) with potassium hydrogen sulfate at 136 C affords 1-(4-imidazolyl)-1-(2,3-dimethyl-phenyl)ethylene (VI), which is finally hydrogenated with H2 over Pd/C in 2N HCl.

参考文献No.77905
标题:Medetomidine
作者:Casta馿r, R.M.; Serradell, M.N.; Casta馿r, J.
来源:Drugs Fut 1987,12(11),1021
合成路线图解说明:

The Grignard condensation of methyl imidazole-4-carboxyate (I) with 2,3-dimethylphenylmagnesium bromide (II) in THF gives 4-(2,3-dimethylbenzoyl) imidazole (III), which (without isolation) is submitted to a new Grignard condensation with methylmagnesium iodide (IV) in the same solvent to yield 1-(4-imidazolyl)-1-(2,3-dimethylphenyl)ethanol (V). The dehydration of (V) with potassium hydrogen sulfate at 136 C affords 1-(4-imidazolyl)-1-(2,3-dimethyl-phenyl)ethylene (VI), which is finally hydrogenated with H2 over Pd/C in 2N HCl.

参考文献No.700068
标题:
作者:Hillier, K.
来源:Acta Univ Oul 1981,8(4),A125
合成路线图解说明:

The Grignard condensation of methyl imidazole-4-carboxyate (I) with 2,3-dimethylphenylmagnesium bromide (II) in THF gives 4-(2,3-dimethylbenzoyl) imidazole (III), which (without isolation) is submitted to a new Grignard condensation with methylmagnesium iodide (IV) in the same solvent to yield 1-(4-imidazolyl)-1-(2,3-dimethylphenyl)ethanol (V). The dehydration of (V) with potassium hydrogen sulfate at 136 C affords 1-(4-imidazolyl)-1-(2,3-dimethyl-phenyl)ethylene (VI), which is finally hydrogenated with H2 over Pd/C in 2N HCl.

参考文献No.802506
标题:Expedient synthesis of 4(5)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, the alpha2-adrenergic agonist medetomidine
作者:Turnbull, S.P.; Kudzma, L.V.
来源:Synthesis 1991,111201
合成路线图解说明:

A new synthesis for medetomidine has been reported: The silylation of N,N-dimethylimidazole-1-sulfonamide (I) with tert-butyldimethylsilyl chloride and butyllithium in THF gives the 2-silyl derivative (II), which is acylated with 2,3-dimethylbenzoyl chloride (III) by means of butyllithium in THF, yielding 2-(tert-butyldimethylsilyl)-5-(2,3-dimethylbenzoyl)-N,N-dimethylimidazo le-1-sulfonamide (IV). Hydrolysis of (IV) with refluxing aqueous HCl affords 5-(2,3-dimethylbenzoyl)imidazole (V), which is finally methylated with methyllithium in THF and reduced with Li in liquid NH3.

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