摘要
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(FTY-720)。方法以苯和正辛酰氯为起始原料,经傅克酰基化、还原、酰化、缩合、还原羰基、还原酯基、去乙酰化和成盐反应得到目的化合物FTY-720,总收率为12.0%。结果与结论目标化合物的结构经1H-NMRI、R和MS确证,中间体的1H-NMR谱和mp值与文献值相符。该合成路线成本低廉,操作简单。
Aim To synthesize the immunosuppressant 2-amino-2- [ 2- （4 octylphenyl） ethyl ]- 1,3-propanediol hydrochloride（FTY-720）. Methods FTY-720 was synthesized via 9 steps using benzene as starting material and total yield was 12 %. Results and conclusion The ^1H-NMR, IR and MS data of the intermediates and the target compound are identical to that of literature. This improved synthetic route is simpler, more efficient and convenient.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第1期33-36,共4页
Chinese Journal of Medicinal Chemistry
