【药物名称】MP-2269
化学结构式(Chemical Structure):
参考文献No.38607
标题:Magnetic resonance blood pool agents
作者:Woulfe, S.R. (Mallinckrodt Medical Inc.)
来源:WO 9820908
合成路线图解说明:

4-Pentylbicyclo[2.2.2]octane-1-carboxylic acid (I) was converted to the corresponding acid chloride with SOCl2 and then coupled to L-aspartic acid beta-tert-butyl ester (II) to afford amide (III). Subsequent coupling of (III) with further L-aspartic acid beta-tert-butyl ester (II) in the presence of DCC and NHS produced diamide (IV). This was then condensed with (aminobutyl)diethylenetriamino-pentaacetic acid penta-tert-butyl ester (V) to provide (VI).

合成路线图解说明:

After deprotection of the tert-butyl ester groups of (VI) with HCl in dioxan, the resulting heptacarboxylic acid (VII) was treated with gadolinium (III) oxide at a controlled pH value to furnish the target gadolinium chelate.

参考文献No.479311
标题:Synthesis and preliminary evaluation of MP-2269: A novel, nonaromatic small-molecule blood-pool MR contrast agent
作者:Wallace, R.A.; Haar, J.P. Jr.; Miller, D.B.; Woulfe, S.R.; Polta, J.A.; Galen, K.P.; Hynes, M.R.; Adzamli, K.
来源:Magn Reson Med 1998,40(5),733
合成路线图解说明:

4-Pentylbicyclo[2.2.2]octane-1-carboxylic acid (I) was converted to the corresponding acid chloride with SOCl2 and then coupled to L-aspartic acid beta-tert-butyl ester (II) to afford amide (III). Subsequent coupling of (III) with further L-aspartic acid beta-tert-butyl ester (II) in the presence of DCC and NHS produced diamide (IV). This was then condensed with (aminobutyl)diethylenetriamino-pentaacetic acid penta-tert-butyl ester (V) to provide (VI).

合成路线图解说明:

After deprotection of the tert-butyl ester groups of (VI) with HCl in dioxan, the resulting heptacarboxylic acid (VII) was treated with gadolinium (III) oxide at a controlled pH value to furnish the target gadolinium chelate.

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