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芬戈莫德合成路线图解 被引量:1

Graphical Synthetic Routes of Fingolimod
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摘要 芬戈莫德(fingolimod,1),化学名为2-氨基-2-[2.(4.正辛基苯基)乙基]-1,3-丙二醇盐酸盐,是诺华公司研发的一种免疫抑制剂,是将子囊菌冬虫夏草的有效成分多球壳菌素(ISP-1)进行结构改造而成,意在减少ISP-1的毒性并改善它的理化性质,并最终明确了其具有免疫抑制活性所必需的化学结构心。
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2013年第1期98-100,共3页 Chinese Journal of Pharmaceuticals
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  • 1王玉成,季,辜顺林,等.一种制备2-对辛基苯乙基-2-氨基丙二醇盐酸盐的方法:中国,1814583A [P].2006-08-09. (CA2006,145: 271380).
  • 2Chiba K, Adachi K. FTY-720, immunosuppressant [J]. DrugsFuture, 1997,22(1): 18-22.
  • 3Adachi K,Kohara T, Nakao N, et al. Design, synthesis, andstructure-activity relationships of 2-substituted-2-amino-1.3-propanediols:discovery of a novel immunosuppressant,FTY720 [J]. Bioorg Med Chem Lett, 1995, 5 (3):853-856.
  • 4Durand P, Peralba P, Sierra F, et al. A new efficient synthesisof the immunosuppressive agent FTY-720 [J]. Synthesis,2000, (4); 505-506.
  • 5Hirase S,Sasaki S, Yoneta M,et al. Process for preparing2-amino-malonic acid derivatives and 2-amino-l,3-propanediol derivatives, and intermediates for preparing thesame: US, 20010008945 [P]. 2001-07-19. (CA 2012, 157:382393).
  • 6Kiuchi M, Adachi K, Kohara T, et al. Synthesis andimmunosuppressive activity of 2-substituted 2-aminopropane-1.3-diolsand 2-aminoethanols [J]. J Med Chem, 2000,43(15):2946-2961.
  • 7Matsumoto N, Hirose R, Sasaki S,et al. Synthesis of the keyintermediate, diethyl 2-acetylamino-2- (2- (4-octanoylphenyl)-ethyl) propane-1,3-dioate, of the immunomodulatory agentFTY720 (Fingolimod) [J]. Chem Pharm Bull, 2008, 56(4):595-597.
  • 8梁铁,路海滨,徐志炳,米浩宇,吴鹏飞,崔磊,王恩思.新型免疫抑制剂FTY-720的合成[J].吉林大学学报(理学版),2008,46(1):139-142. 被引量:8

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