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【结 构 式】

【分子编号】13351

【品名】1,2-Bis(aminomethyl)cyclobutane diacqua platinum complex dinitrate

【CA登记号】

【 分 子 式 】C6H14N2Pt

【 分 子 量 】309.27064

【元素组成】C 23.3% H 4.56% N 9.06% Pt 63.08%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(V)

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.

1 Aulenbacher, P.; Engel, J.; Hilgard, P.; Gunther, E.; Voegeli, R.; Lobaplatin. Drugs Fut 1992, 17, 10, 883.
2 Schumacher, W.; Engel, J.; Respondek, J.; Voegeli, R.; Hilgard, P.; D-19466, a new cyclobutane-platinum complex with antitumor activity. J Cancer Res Clin Oncol 1990, 116, 5, 439-42.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(II-b) 13347 1,2-Cyclobutanedicarbonitrile; trans-Cyclobutane-1,2-dicarbonitrile 3211-20-9 C6H6N2 详情 详情
(II-a) 63575 (1R,2S)-1,2-cyclobutanedicarbonitrile C6H6N2 详情 详情
(I) 10848 2-Ethyl-2-(4-pyridinyl)pentanedinitrile C12H13N3 详情 详情
(III) 13348 [2-(Aminomethyl)cyclobutyl]methylamine; [2-(Aminomethyl)cyclobutyl]methanamine C6H14N2 详情 详情
(IV) 13349 1,2-Bis(aminomethyl)cyclobutane dichloro platinum complex C6H14Cl2N2Pt 详情 详情
(V) 13351 1,2-Bis(aminomethyl)cyclobutane diacqua platinum complex dinitrate C6H14N2Pt 详情 详情
Extended Information