【药物名称】Lobaplatin, D-19466
化学结构式(Chemical Structure):
参考文献No.131611
标题:D-19466, a new cyclobutane-platinum complex with antitumor activity
作者:Voegeli, R.; Schumacher, W.; Engel, J.; Respondek, J.; Hilgard, P.
来源:J Cancer Res Clin Oncol 1990,116(5),439-42
合成路线图解说明:

The synthesis of the ligand begins with a thermal or photochemical head-to-head dimerization of acrylonitrile (I). The mixture of the resulting cis- and trans-1,2-cyclobutanedicarbonitrile(II a-b) is separated by distillation and the trans-compound (II b) is then transformed to 1,2-bis(aminomethyl)cyclobutane (III) by reduction with lithiumalanat. The dichloroplatinum complex (IV) is conveniently prepared from diamine (III) and potassium tetrachloroplatinate. This complex reacts with silver nitrate to give the nitrato-complex (V), which was not isolated. After passing through a column of a strong anion exchanger in the OH-form, the activated complex reacts in aqueous solution with L-lactic acid to form the lactato-complex D-19466 as a diastereomeric mixture. The general reaction sequence is outlined in scheme 14986401a.

参考文献No.183955
标题:Lobaplatin
作者:Aulenbacher, P.; Engel, J.; Hilgard, P.; G黱ther, E.; Voegeli, R.
来源:Drugs Fut 1992,17(10),883
合成路线图解说明:

The synthesis of the ligand begins with a thermal or photochemical head-to-head dimerization of acrylonitrile (I). The mixture of the resulting cis- and trans-1,2-cyclobutanedicarbonitrile(II a-b) is separated by distillation and the trans-compound (II b) is then transformed to 1,2-bis(aminomethyl)cyclobutane (III) by reduction with lithiumalanat. The dichloroplatinum complex (IV) is conveniently prepared from diamine (III) and potassium tetrachloroplatinate. This complex reacts with silver nitrate to give the nitrato-complex (V), which was not isolated. After passing through a column of a strong anion exchanger in the OH-form, the activated complex reacts in aqueous solution with L-lactic acid to form the lactato-complex D-19466 as a diastereomeric mixture. The general reaction sequence is outlined in scheme 14986401a.

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