论文部分内容阅读
D(-)-酒石酸二乙酯(1)分别与2-氨甲基吡啶和4-氨甲基吡啶反应,合成了D(-)-二吡啶甲基酒石酸酰胺2和3.分别以1～3为手性配体与钛酸异丙酯配合,催化过氧化氢异丙苯(CHP)不对称氧化埃索美拉唑前体(Eso-I)合成埃索美拉唑.结果表明,由配体2或3构成的催化体系在埃索美拉唑合成上显示出较高的催化活性和对映选择性.例如,当以2为配体,甲苯为溶剂,在优化的条件下进行反应时,Eso-I的转化率达84.7%,埃索美拉唑的选择性达91.8%,对映体过量值达89.0%.
D - (-) - dipyridyl methyl tartaric acid amide 2 and D (-) - diphosphonic acid tartaric acid amide 2 were synthesized by reaction with 2-aminomethylpyridine and 4-aminomethylpyridine, respectively. 3 is a chiral ligand with isopropyl titanate to catalyze the asymmetric oxidation of esomeprazole (Eso-I) with cumene hydroperoxide (CHP) to synthesize esomeprazole.The results showed that The catalytic system composed of ligand 2 or 3 shows higher catalytic activity and enantioselectivity in the synthesis of esomeprazole.For example, when 2 is a ligand, toluene is used as a solvent and the reaction is carried out under optimized conditions , The conversion rate of Eso-I was 84.7%, the selectivity of esomeprazole was 91.8%, and the enantiomeric excess was 89.0%.