新型免疫抑制剂FTY-720的合成  

Synthesis of a New Immunosuppressant FTY-720

作　　者：梁铁[1] 路海滨[2] 徐志炳[2] 米浩宇[2] 吴鹏飞[3] 崔磊[3] 王恩思[2] 

机构地区：[1]长春中医药大学附属医院,长春130061 [2]吉林大学生命科学学院,长春130021 [3]吉林大学药学院,长春130021

出　　处：《吉林大学学报（理学版）》2008年第1期139-142,共4页Journal of Jilin University:Science Edition

基　　金：吉林省科技厅科技发展计划项目基金(批准号:20020503-11)

摘　　要：分别以苯为原料,经傅克酰基化、还原、酰化、缩合、还原羰基、还原酯基、去乙酰化、成盐反应和以苯乙醇为原料,经氯化、傅克酰基化、缩合、还原羰基、还原酯基、去乙酰化、成盐反应合成目标分子FTY-720,总收率分别为17%和21%.各关键中间体及FTY-720的结构经红外光谱、核磁共振氢谱及碳谱、质谱等得到确证.FFY-720, a new kind of immunosuppressant, 2-amino-2 [ 2-（4-octylphenyl） ethyl ] -1,3-propanediol hydrochloride was synthesized via Friedel-crafts acylation, reduction, acylation, alkylation and Et3 Sill/TiCl4 reduction as a pivotal step from the starting material benzene or Friedel-crafts acylation, alkylation, Et3 Sill/TiCl, reduction and reduction as a pivotal step from the starting material phenethyl alcohol respectively and the total yield of the FTY-720 was 17% or 21% respectively. The structure of the target molecule and the key intermediates were confirmed by IR, ^1H NMR, ^13C NMR and MS in our experiments. The route is simpler, more efficient and convenient that may be applied to industrial production.

关 键 词：合成 FTY-720 药物化学 免疫抑制剂 

分 类 号：O621.26[理学—有机化学]