【药物名称】Tirilazad mesylate, ISV-600, U-74006F, Tridax, Freedox
化学结构式(Chemical Structure):
参考文献No.101095
标题:THE 21-AMINOSTEROIDS: POTENT INHIBITORS OF LIPID PEROXIDATION FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM TRAUMA AND ISCHEMIA
作者:Braughler, J.M.; Hall, E.D.; Jacobsen, E.J.; McCall, J.M.; Means, E.D.
来源:Drugs Fut 1989,14(2),143
合成路线图解说明:

The intermediate pyrimidine (IV) has been obtained as follows: The reaction of 2,4,6-trichloropyrimidine (I) with pyrrolidine in THF gives 6-chloro-2,4-bis(1-pyrrolidinyl) pyrimidine (II), which is condensed with piperazine (III) in pyridine to yield 6-(1-piperazinyl)-2,4-bis(1-pyrrolidinyl)pyrimidine (IV). The methylation of 21-acetoxy-pregna-1,4,9(11),16-tetraene-3,20-dione (V) with methylmagnesium chloride catalyzed by copper propionate, followed by hydrolysis of the acetate group with NaOMe in methanol, gives the 16-alpha-methyl steroid (VI), which is condensed with piperazine intermediate (IV) by means of MeSO2Cl and TEA in acetonitrile, affording the precursor (VII). Finally, this compound is treated with methanesulfonic acid to afford the target compound.

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