【药物名称】DP-BAPTA-99, DP-b99
化学结构式(Chemical Structure):
参考文献No.51927
标题:Lipophilic diesters of chelating agents
作者:Kozak, A.; Shapiro, I. (D-Pharm Ltd.)
来源:JP 2001518458; WO 9916741
合成路线图解说明:

By condensation of 4-(4-fluorophenyl)-3-(hydroxymethyl)piperidine (I) with 3,4-methylenedioxyphenol (II) with dicyclohexylcarbodiimide (DCC) at 180 C.

合成路线图解说明:

Treatment of 1,2-bis-(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (I) with acetic anhydride and pyridine provided the cyclic anhydride (II). Ethylene glycol octyl ether (V) was prepared by Williamson's synthesis from the sodium alkoxide of ethylene glycol (III) and n-octyl bromide (IV). Finally, the title diester was obtained by heating anhydride (II) with the octyl ether of ethyleneglycol (V).

合成路线图解说明:

Treatment of bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (I) with acetic anhydride in hot pyridine produced the cyclic anhydride (II). Ethyleneglycol mono-ether (V) was prepared by Williamson's synthesis from the sodium alkoxide of ethylene glycol (IV) and octadecyl bromide (III). Then, heating the bis-anhydride (II) with ethyleneglycol monoether (V) produced the title diester

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