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【结 构 式】

【药物名称】Tibezonium iodide

【化学名称】N,N-Diethyl-N-methyl-2-[4-[4-(phenylsulfanyl)phenyl]-3H-1,5-benzodiazepin-2-ylsulfanyl]ethanaminium iodide

【CA登记号】54663-47-7

【 分 子 式 】C28H32IN3S2

【 分 子 量 】601.61974

【开发单位】

【药理作用】 

合成路线1

The reaction of 4-acetyldiphenylsulfide (I) with carbon disulfide by means of sodium tert-amyloxide in benzene gives 4-phenylthiobenzoyldithioacetic acid (II), which is cyclized with o-phenylenediamine (III) in refluxing toluene yielding 4-(p-phenylthiophenyl)-1,3-dihydro-2H-1,5-benzodiazepine-2-thione (IV). The condensation of (IV) with diethylaminoethyl chloride (V) by means of NaH in refluxing benzene affords 2-[beta-(N-diethylamino)ethylthio]-4-(p-phenylthio)phenyl-3H-1,5-benzodiazepine (VI), which is finally quaternized with methyl iodide in isopropanol. (1,2)

1 Castaner, J.; de Angelis, L.; Tibezonium Iodide. Drugs Fut 1978, 3, 2, 152.
2 Nardi, D.; et al.; New 2-methyldialkylammoniumalkylthio-4-p-substituted phenyl-3-H-1,5-benzodiazepine iodides with antibacterial activity. II Farmaco (ed. sc.) 1975, 30, Suppl. 3, 248.
3 Degen, L. (Recordati S.A. Chem Pharm. Co.); AT 321922; CH 555347; GB 1412008; GB 1412009; US 3993793 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 60710 1-[4-(phenylsulfanyl)phenyl]-1-ethanone C14H12OS 详情 详情
(II) 60711 3-oxo-3-[4-(phenylsulfanyl)phenyl]propanedithioic acid C15H12OS3 详情 详情
(III) 12324 methyl (2R)-2-amino-3-phenylpropanoate 21685-51-8 C10H13NO2 详情 详情
(IV) 60712 4-[4-(phenylsulfanyl)phenyl]-1,3-dihydro-2H-1,5-benzodiazepine-2-thione C21H16N2S2 详情 详情
(V) 16194 2-chloro-N,N-diethyl-1-ethanamine; N-(2-chloroethyl)-N,N-diethylamine 100-35-6 C6H14ClN 详情 详情
(VI) 60713 N,N-diethyl-2-({4-[4-(phenylsulfanyl)phenyl]-3H-1,5-benzodiazepin-2-yl}sulfanyl)-1-ethanamine; N,N-diethyl-N-[2-({4-[4-(phenylsulfanyl)phenyl]-3H-1,5-benzodiazepin-2-yl}sulfanyl)ethyl]amine C27H29N3S2 详情 详情
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