α-甲氨基-苄基亚膦酸及其酯类化合物的合成  

Synthesis of α-Methylaminobenzyl-phosphonic Acid and Phosphite Compounds

作　　者：赵承[1] 田桂杰[1] 林浩[1] 王德心[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《中国药物化学杂志》2000年第4期266-269,共4页Chinese Journal of Medicinal Chemistry

摘　　要：利用类似Arbuzov反应及Mannich反应设计合成了 12种α (甲氨基 ) 苄基亚膦酸类化合物和 2种α (甲氨基 ) 苄基亚膦酸酯类化合物 .它们的结构均经MS或1H NMR证明 .其中 12种亚膦酸化合物由取代的苯甲醛、甲胺及亚膦酸为底物 ,以环丁砜为溶剂 ,TsOH为催化剂 ,缩合而成 .此法的优点为易于纯化 .另 2种亚膦酸酯化合物以相应的芳醛、甲胺及亚膦酸二乙酯为底物 ,以无水乙醇为溶剂 ,经Mannich反应缩合而得 .此法操作简便 ,收率高于前者 .Fourteen benzyl phosphonic acid derivatives were synthesized via the Arbuzov type reaction or Mannich condensation.Their structures were confirmed by FAB or ESI (2a 2k) or 1H NMR(4,7,8).Among the title compounds free α methylamino benzyl phosphonic acid compounds were prepared directly from substituted benzaldehyde,methylamine and phosphorous acid,using tetramethylenesulfone as the solvent and TsOH as the catalyst.This procedure offered the advantage of easy purification of the products.Ethyl (α methylamino benzyl )phosphites were prepared from substituted benzaldehyde or benzoheterocyclic aldehyde,methylamine and diethyl phosphite,using anhydrous ethanol as the solvent.This method is convenient,simple and gives good yield.

关 键 词：苄膦酸(酯) Arbuzov反应 MANNICH反应 合成 

分 类 号：R914[医药卫生—药物化学]