一种新型免疫调节剂SYL927的合成方法研究  

Synthesis of a novel immunomodulator SYL927

作　　者：肖琼[1] 林成刚 汪小涧[1] 尹大力[1] 

机构地区：[1]中国医学科学院/北京协和医学院药物研究所活性物质发现与适药化北京市重点实验室,北京100050 [2]南京诺瑞特医药科技有限公司,江苏南京210000

出　　处：《中国药物化学杂志》2016年第4期307-312,共6页Chinese Journal of Medicinal Chemistry

基　　金：十二五重大新药创制科技重大专项(2012ZX09301002-001)

摘　　要：目的报道一种新型免疫调节剂SYL927的合成方法。方法以联苯为起始原料,经酰化、缩合、还原、傅克酰化、成酯、环合、还原、碱水解、成盐共9步反应制得SYL927;其结构经1H-NMR、13C-NMR和MS谱确证。结果与结论改进了目标物的合成方法,使之更适合工业生产要求,总收率为14.4%。同时分析了环合反应副产物生成的原因,并对副产物进行了结构鉴定。We report the synthetic method of a novel immunomodulator SYL927.It was prepared from phenylbenzene by a nine-step reaction,including acylation,condensation,reduction,Friedel-Crafts acylation,esterification,cyclization,reduction,hydrolysis and salt forming reaction with the overall yield of 14.4%.Particularly,we indentified the structure of the by-product generated in the cyclization reaction and get to knowhowit was generated.Sequencely,we made a process improvement on the cyclization reaction and improved the quality of final product.The structure of SYL927 was confirmed by1H-NMR,13C-NMR and MS.

关 键 词：SYL927 S1P1受体 免疫调节 合成 

分 类 号：R914.5[医药卫生—药物化学]