Pentamorphone, A-4492, RX-77989-药物合成数据库

【药物名称】Pentamorphone, A-4492, RX-77989

化学结构式(Chemical Structure):

参考文献No.	8332
标题:	Morphine derivs., process for their preparation and medicines containing them
作者:	Kobylecki, R.J.; Guest, I.G.; Lewis, J.W.; Kirby, G.W. (Reckitt & Colman Pharmaceuticals)
来源:	DE 2812581

合成路线图解说明: The reduction of 14beta-nitrocodeinone dimethylketal (I) with AlCl3-Zn and ammonium chloride in refluxing methanol gives 14beta-aminocodeinone dimethylketal (II), which is acylated with pentanoyl chloride and triethylamine in hot chloroform yielding 14beta-(pentanoylamino)codeinone dimethylketal (III). The reduction of (III) with LiAlH4 in THF affords 14beta-(pentylamino)codeinone (IV), which is finally demethylated by treatment with boron trichloride in methylene chloride at -30 C.

参考文献No.	101819
标题:	PENTAMORPHONE
作者:	Prous, J.; Casta馿r, J.
来源:	Drugs Fut 1990,15(4),352

合成路线图解说明: The reduction of 14beta-nitrocodeinone dimethylketal (I) with AlCl3-Zn and ammonium chloride in refluxing methanol gives 14beta-aminocodeinone dimethylketal (II), which is acylated with pentanoyl chloride and triethylamine in hot chloroform yielding 14beta-(pentanoylamino)codeinone dimethylketal (III). The reduction of (III) with LiAlH4 in THF affords 14beta-(pentylamino)codeinone (IV), which is finally demethylated by treatment with boron trichloride in methylene chloride at -30 C.