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Spirogermanium hydrochloride, SG, NSC-192965, Spiro-32

锗螺胺Chemical Name: 8,8-Diethyl-N,N-dimethyl-2-aza-8-germaspiro[4.5]decane-2-propanamine dihydrochloride; N-(3-Dimethylaminopropyl)-2-aza-8,8-diethyl-8-germaspiro[4.5]decane dihydrochloride
CAS No. 41992-22-7, 41992-23-8 (free base)
项目整合开发状态: Phase II
项目研究机构: Unimed (Originator)
合成路线:The condensation of diethylgermanium dihydride (I) with methyl acrylate (II) gives diethyldi-(beta-carbomethoxyethyl)germane (III),which is cyclized by treatment with potassium tert-butoxide in refluxing toluene yielding carbomethoxy-4,4-diethyl-4-germacyclohexanone (IV).The decarboxylative hydrolysis of (IV) with refluxing 20% aqueous H2SO4 affords 4,4-diethyl-4-germacyclohexanone (V),which is condensed with ethyl cyanoacetate (VI) by means of ammonium acetate acetic acid in refluxing benzene giving ethyl alpha-cyano-alpha-(4,4-diethyl-4-germacyclohexylidene)acetate (VII).The treatment of (VII) with KCN in ethanol-water,and then with refluxing aqueous HCl yields 4,4-diethyl-4-germacyclohexane-1-carboxy-1-acetic acid (VIII),which is then converted into its cyclic anhydride (IX) by reaction with refluxing acetic anhydride.The reaction of (IX) with 3-dimethylaminopropylamine (X) at 180 C gives N-(3-dimethylaminopropyl)-2-aza-8,8-diethyl-8-germaspiro[4.5]decane-1,3-dione (XI),which is finally reduced with LiAlH4 in benzene-ether.
📌 参考资料/链接:
参考文献标题:Spirogermanium Hydrochloride
文献作者:Castar,J.
参考来源:Drugs Fut 1980,5(3),149

📄 详细内容


合成路线:The condensation of diethylgermanium dihydride (I) with methyl acrylate (II) gives diethyldi-(beta-carbomethoxyethyl)germane (III),which is cyclized by treatment with potassium tert-butoxide in refluxing toluene yielding carbomethoxy-4,4-diethyl-4-germacyclohexanone (IV).The decarboxylative hydrolysis of (IV) with refluxing 20% aqueous H2SO4 affords 4,4-diethyl-4-germacyclohexanone (V),which is condensed with ethyl cyanoacetate (VI) by means of ammonium acetate acetic acid in refluxing benzene giving ethyl alpha-cyano-alpha-(4,4-diethyl-4-germacyclohexylidene)acetate (VII).The treatment of (VII) with KCN in ethanol-water,and then with refluxing aqueous HCl yields 4,4-diethyl-4-germacyclohexane-1-carboxy-1-acetic acid (VIII),which is then converted into its cyclic anhydride (IX) by reaction with refluxing acetic anhydride.The reaction of (IX) with 3-dimethylaminopropylamine (X) at 180 C gives N-(3-dimethylaminopropyl)-2-aza-8,8-diethyl-8-germaspiro[4.5]decane-1,3-dione (XI),which is finally reduced with LiAlH4 in benzene-ether.

参考文献标题:
文献作者:Rice,L.M.
参考来源:US 3825546


合成路线:The condensation of diethylgermanium dihydride (I) with methyl acrylate (II) gives diethyldi-(beta-carbomethoxyethyl)germane (III),which is cyclized by treatment with potassium tert-butoxide in refluxing toluene yielding carbomethoxy-4,4-diethyl-4-germacyclohexanone (IV).The decarboxylative hydrolysis of (IV) with refluxing 20% aqueous H2SO4 affords 4,4-diethyl-4-germacyclohexanone (V),which is condensed with ethyl cyanoacetate (VI) by means of ammonium acetate acetic acid in refluxing benzene giving ethyl alpha-cyano-alpha-(4,4-diethyl-4-germacyclohexylidene)acetate (VII).The treatment of (VII) with KCN in ethanol-water,and then with refluxing aqueous HCl yields 4,4-diethyl-4-germacyclohexane-1-carboxy-1-acetic acid (VIII),which is then converted into its cyclic anhydride (IX) by reaction with refluxing acetic anhydride.The reaction of (IX) with 3-dimethylaminopropylamine (X) at 180 C gives N-(3-dimethylaminopropyl)-2-aza-8,8-diethyl-8-germaspiro[4.5]decane-1,3-dione (XI),which is finally reduced with LiAlH4 in benzene-ether.
参考文献标题:Spirans.XXII.Synthesis of 4,4-dialkyl-4-germacyclohexanone and 8,8-dialkyl-8-germaazaspiro[4,5]decanes
文献作者:Rice,L.M.; et al.
参考来源:J Heterocycl Chem 1974,11(6),1041-47


产品链接: CAS No. 41992-22-7››

产品链接: CAS No.41992-23-8››