新型免疫抑制剂2-氨基-2-[2-(4-正辛基苯基)乙基]-1,3-丙二醇盐酸盐(FTY720)的合成

Synthesis of a new immunosuppressant 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride(FTY720)

目的合成新型免疫抑制剂2-氨基-2-[2-(4-正辛基苯基)乙基]-1,3-丙二醇盐酸盐(FTY720)。方法以氯化苄和溴代正庚烷为起始原料,经W urtz偶联、氯乙酰化、缩合、羰基还原、酯基还原、去乙酰化和成盐反应得到目标化合物FTY720,总收率为22.5%。结果与结论目标化合物的结构经1H-NMR1、3C-NMR和MS确证。中间体的1H-NMR谱和熔点与文献值相符。该合成路线成本低廉,步骤较短,操作简单。

Aim To synthesize the immunosuppressant 2-amino-2-（ 2-（4-octylphenyl ） ethyl ） -1,3-propanediol hydrochloride （FTY720）. Methods FTY-720 was synthesized via 7 steps using benzyl chloride and 1-bromo- heptane as starting materials and total yield was 22. 5%. Results and conclusion The ^1H-NMR, ^13C-NMR and MS data of the intermediates and FTY720 are identical to that of literature. This improved synthetic route is simpler, more efficient and convenient.