新型（1-烷酰氧基-4-烷酰氨基亚丁基）-1,1-二膦酸衍生物的合成

Turhanen Petri A, Vepsäläinen Jouko J

University of Kuopio, Department of Chemistry, P,O, Box 1627, FIN-70211, Kuopio, Finland.

Beilstein J Org Chem. 2006 Feb 24;2(1):2. doi: 10.1186/1860-5397-2-2.

A novel strategy for the synthesis of (1-alkanoyloxy-4-alkanoylaminobutylidene)-1,1-bisphosphonic acid derivatives (1a-d) via (1-hydroxy-4-alkanoylaminobutylidene)-1,1-bisphosphonic acid derivatives (2a-d), starting from alendronate has been developed with reasonable 51-77% overall yields. Intermediate products, (1-hydroxy-4-alkanoylaminobutylidene)-1,1-bisphosphonic acid derivatives (2a-d), were prepared in water with reasonable to high yields (52-94%).

已开发出一种从阿仑膦酸盐出发，经由（1-羟基-4-烷酰氨基丁叉基）-1,1-双膦酸衍生物（2a-d）合成（1-烷酰氧基-4-烷酰氨基丁叉基）-1,1-双膦酸衍生物（1a-d）的新策略，总产率合理，为51-77%。中间产物（1-羟基-4-烷酰氨基丁叉基）-1,1-双膦酸衍生物（2a-d）在水中制备，产率合理至高（52-94%）。