论文部分内容阅读
化学名顺-(2,2-二氨基甲基-1,3-丙二醇-N,N)[1,1-环丁烷二羧酸(2-)-O,O′]铂(Ⅱ) 合成本品有两条合成路线: 1.四氯代铂酸钾(Ⅰ)与二甲亚砜反应生成双(二甲亚砜-S,S′)-二氯合铂(Ⅱ),然后与1,1-环丁烷二羧酸银(Ⅲ)缩合得双(二甲亚砜-S,S′)(1,1-环丁烷二羧酸-O,O′)-铂(Ⅳ),最后在回流水中用2,2-双(氨基甲基)-1,3-丙二醇(Ⅴ)处理Ⅳ,即得本品。 2.四氯代铂酸钾(Ⅰ)与二胺(Ⅴ)反应得(2,2-双(氨基甲基)-1,3-丙二醇-N,N′]二氯合铂(Ⅵ),然后用银盐如上处理制得本品。Ⅴ由2,2-二溴甲基-1,3-丙二醇(Ⅶ)与叠氮化物在热DMF中反应得2,2-二叠氮甲基-1,3-丙二醇(Ⅷ),然后用H_2和Pt/C还原制得。药理作用Zenipatin是一种水溶性的第三代铂络合物,抗小鼠P388白血病有良好
Synthesis of (1,1-cyclobutanedicarboxylic acid (2 -) - O, O ’] platinum (Ⅱ) with cis- (2,2-diaminomethyl-1,3-propanediol- This product has two synthetic routes: 1. Potassium tetrachloroplatinate (Ⅰ) and dimethyl sulfoxide reaction of bis (dimethyl sulfoxide -S, S ’) - dichloro platinum (Ⅱ), and then with 1 (1,1-cyclobutanedicarboxylic acid-O, O ’) -platinum (IV) is obtained by condensation of silver (III) 1- cyclobutanedicarboxylate with Finally in refluxing water with 2,2-bis (aminomethyl) -1,3-propanediol (Ⅴ) treatment Ⅳ, to obtain the goods. 2. Reaction of platinum tetrachloro-platinum (Ⅰ) with diamine (Ⅴ) gave (2,2-bis (aminomethyl) -1,3-propanediol-N, Then the silver salt was treated as above to obtain the goods.V 2,2-dibromomethyl-1,3-propanediol (VII) and azide reaction in hot DMF 2,2-diazidomethyl- 1,3-propanediol (Ⅷ) and then reduced with H 2 and Pt / C pharmacological effects Zenipatin is a water-soluble third generation platinum complex that has good anti-mouse P388 leukemia