新型骨吸收抑制剂唑来膦酸的合成

Synthesis of Zoledronate

以咪唑为起始原料 ,和溴乙酸乙酯经 N-烷基化、水解、成盐得 2 -( 1 -咪唑基 )乙酸盐酸盐 ( 4 ) ,4再与三氯化磷的氯苯溶液反应得唑来膦酸。总收率 2 5 .4 % (以咪唑计 )。

Zoledronate was synthesized from imidazole via N-alkylation with ethyl bromoacetate, hydrolysis, salification to give 2-(1-imidazolyl)acetic acid hydrochloride which was reacted with PCl 3 in chlorobenzene. The overall yield was about 25.4%.