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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 2-amino-2- [2- (4-n-octylphenyl) ethyl] -1,3-propanediol hydrochloride (FTY720) as a novel immunosuppressant. Methods Starting from benzyl chloride and n-heptane bromide, the target compound FTY720 was obtained via Würtz coupling, chloroacetylation, condensation, carbonyl reduction, ester reduction, deacetylation and salt formation. The overall yield Is 22.5%. Results and Conclusions The structures of target compounds were confirmed by 1H-NMR1,3C-NMR and MS. The 1H-NMR spectra and melting points of the intermediates are consistent with those of the literature. The synthetic route has the advantages of low cost, short steps and simple operation.