2-(4’,4’-二膦酸基)丁酰氨基-3-(4-’N,N-二(β-氯乙基)氨基)苯基-丙酸的合成及初步的骨靶向性研究

作者：陈沛; 张涛; 范琴; 曾建成; 吴勇

来源：四川大学学报(自然科学版), 2006, 43(03): 706-709.

DOI：10.3969/j.issn.0490-6756.2006.03.047

• 4,4-bis(diethoxyphosphono)-butyric acid
• synthesis
• Melphalan
• bone-targeting

The immediate(3) was prepared via three steps: at first substitutionof diethyl phosphonite,as the initial material,followed by addition-elimination.After Michael Reaction withdiethylmalonate,hydrolyzation and decarboxylation,(3) converted into key immediate(6),which was subsequentlyconjugated with Melphalan and specifically phosphonate cleaved.Then thetitle conjugate Awas achieved.Its structure was verified by()~(1)HNMR,IR,MS and it showed good bone targeting ability via hydroxyapatite adhesion testsin vitro.

• 单位
  四川大学; 四川大学华西医院