【药物名称】YM17E
化学结构式(Chemical Structure):
参考文献No.10857
标题:Diurea derivatives useful as medicaments and processes for the preparation thereof
作者:Ito, N.; Yasunaga, T.; Iizumi, Y.; Araki, T. (Yamanouchi Pharmaceutical Co., Ltd.)
来源:AU 8928669; EP 0325397; JP 1990117651; US 5091419; US 5166429; US 5384425
合成路线图解说明:

Reaction of isophthaloyl dichloride (I) with cycloheptylamine (II) in the presence of triethylamine in dichloromethane gives N,N'-dicycloheptylisophthalimide (III), which is reduced with sodium bis(2-methoxyethoxy)aluminum hydride in toluene to yield 1,3-bis(cycloheptylaminomethyl)benzene (IV). Compound (IV) is treated with p-nitrophenylisocyanate (V) to afford 1,3-bis[1-cycloheptyl-3-(4-nitrophenyl)ureidomethyl]benzene (VI), which is reduced with hydrogen in the presence of palladium over charcoal to give 1,3-bis[1-cycloheptyl-3-(4-aminophenyl)ureidomethyl]benzene (VII). Finally, compound (VII) is treated with aqueous formaldehyde and hydrogen in the presence of platinum oxide in ethanol, followed by addition of hydrochloric acid in ethanol.

参考文献No.160478
标题:Synthesis and hypocholesterolemic activity of phenylene and pyridylene diurea derivatives as ACAT inhibitors
作者:Iizumi, Y.; Ohhata, I.; Iwaoka, K.; Matsuda, K.; Ito, N.; Yasunaga, T.; Araki, T.
来源:202nd ACS Natl Meet (Aug 25-30, New York) 1991,Abst MEDI 109
合成路线图解说明:

Reaction of isophthaloyl dichloride (I) with cycloheptylamine (II) in the presence of triethylamine in dichloromethane gives N,N'-dicycloheptylisophthalimide (III), which is reduced with sodium bis(2-methoxyethoxy)aluminum hydride in toluene to yield 1,3-bis(cycloheptylaminomethyl)benzene (IV). Compound (IV) is treated with p-nitrophenylisocyanate (V) to afford 1,3-bis[1-cycloheptyl-3-(4-nitrophenyl)ureidomethyl]benzene (VI), which is reduced with hydrogen in the presence of palladium over charcoal to give 1,3-bis[1-cycloheptyl-3-(4-aminophenyl)ureidomethyl]benzene (VII). Finally, compound (VII) is treated with aqueous formaldehyde and hydrogen in the presence of platinum oxide in ethanol, followed by addition of hydrochloric acid in ethanol.

参考文献No.160479
标题:Synthesis and activity of a novel phenylenediurea derivative with hypolipidemic and antiatherosclerotic activity
作者:Yasunaga, T.; Araki, T.; Iwaoka, K.; Iizumi, Y.; Ohata, I.; Matsuda, K.; Ito, N.
来源:111th Annu Meet Pharmaceut Soc Jpn (March 28-30, Tokyo) 1991,Abst 29V 3-040.
合成路线图解说明:

Reaction of isophthaloyl dichloride (I) with cycloheptylamine (II) in the presence of triethylamine in dichloromethane gives N,N'-dicycloheptylisophthalimide (III), which is reduced with sodium bis(2-methoxyethoxy)aluminum hydride in toluene to yield 1,3-bis(cycloheptylaminomethyl)benzene (IV). Compound (IV) is treated with p-nitrophenylisocyanate (V) to afford 1,3-bis[1-cycloheptyl-3-(4-nitrophenyl)ureidomethyl]benzene (VI), which is reduced with hydrogen in the presence of palladium over charcoal to give 1,3-bis[1-cycloheptyl-3-(4-aminophenyl)ureidomethyl]benzene (VII). Finally, compound (VII) is treated with aqueous formaldehyde and hydrogen in the presence of platinum oxide in ethanol, followed by addition of hydrochloric acid in ethanol.

参考文献No.217620
标题:YM17E
作者:Graul, A.; Casta馿r, J.; Prous, J.
来源:Drugs Fut 1993,18(9),813
合成路线图解说明:

Reaction of isophthaloyl dichloride (I) with cycloheptylamine (II) in the presence of triethylamine in dichloromethane gives N,N'-dicycloheptylisophthalimide (III), which is reduced with sodium bis(2-methoxyethoxy)aluminum hydride in toluene to yield 1,3-bis(cycloheptylaminomethyl)benzene (IV). Compound (IV) is treated with p-nitrophenylisocyanate (V) to afford 1,3-bis[1-cycloheptyl-3-(4-nitrophenyl)ureidomethyl]benzene (VI), which is reduced with hydrogen in the presence of palladium over charcoal to give 1,3-bis[1-cycloheptyl-3-(4-aminophenyl)ureidomethyl]benzene (VII). Finally, compound (VII) is treated with aqueous formaldehyde and hydrogen in the presence of platinum oxide in ethanol, followed by addition of hydrochloric acid in ethanol.

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