【药物名称】Minaxolone
化学结构式(Chemical Structure):
参考文献No.701427
标题:
作者:Philips, G.H.; Ewan, G.
来源:DE 2715078
合成路线图解说明:

The ketalization of 2beta-ethoxy-3alpha-hydroxy-5alpha-pregnane-11,20-dione (I) with ethylene glycol (A) by means of p-toluenesulfonic acid in refluxing benzene gives the corresponding 20,20-ethylenedioxy derivative (II), which is treated with hydroxylamine hydrochloride and NaOH refluxing ethanol to yield 20,20-ethylenedioxy-2beta-ethoxy-3alpha-hydroxy-5alpha-pregnan-11-one 11-oxime (III). The reduction of (III) with Na in refluxing propanol (B) affords 11alpha-amino-20,20-ethylenedioxy-2beta-ethoxy-3alpha-hydroxy-5alpha-pregnan (IV), which is finally methylated with methyl iodide and K2CO3 or with formaldehyde and formic acid, and hydrolyzed with HCl or H2SO4.

参考文献No.800501
标题:Minaxolone
作者:Hillier, K.; Casta馿r, J.; Blancafort, P.; Serradell, M.N.
来源:Drugs Fut 1980,5(12),614
合成路线图解说明:

The ketalization of 2beta-ethoxy-3alpha-hydroxy-5alpha-pregnane-11,20-dione (I) with ethylene glycol (A) by means of p-toluenesulfonic acid in refluxing benzene gives the corresponding 20,20-ethylenedioxy derivative (II), which is treated with hydroxylamine hydrochloride and NaOH refluxing ethanol to yield 20,20-ethylenedioxy-2beta-ethoxy-3alpha-hydroxy-5alpha-pregnan-11-one 11-oxime (III). The reduction of (III) with Na in refluxing propanol (B) affords 11alpha-amino-20,20-ethylenedioxy-2beta-ethoxy-3alpha-hydroxy-5alpha-pregnan (IV), which is finally methylated with methyl iodide and K2CO3 or with formaldehyde and formic acid, and hydrolyzed with HCl or H2SO4.

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